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We present an improved and convenient synthesis of [2.2]paracyclophane-imidazoline N,O-ligands with central and planar chirality in seven steps starting from [2.2]paracyclophane. The utility of these ligands in organozinc additions to aldehydes is described. The asymmetric ethylation of aldehydes proceeded with enantioselectivities of up to 97 % ee, while the asymmetric arylation of aldehydes gave up to 95 % ee (R) and 82 % ee (S) using (S,S,S P )-UCD-Imphanol and (S,S,R P )-UCD-Imphanol, respectively., (© 2024 The Author(s). Chemistry - A European Journal published by Wiley-VCH GmbH.)

Oxa- and azabicyclic alkenes can be readily activated by transition-metal complexes with facial selectivity, because of the intrinsic reactivity of strained bicyclic structures. Synthetically, these compounds are important synthons that offer an important platform for the construction of biologically/medicinally significant compounds with two or more stereocenters. This Review comprehensively compiles the diverse catalytic processes involving the enantioselective transformations of oxa- and azabicyclic alkenes. It has been organized according to reaction type, including asymmetric ring opening (ARO) reactions, hydrofunctionalizations, cycloadditions and C-H activation reactions. The ARO section has been subdivided based on the type of nucleophiles employed, and further subdivided based on the metal used, with a separate topic dedicated to asymmetric ring-opening metathesis. Lastly, the presentation of each method/group of reactions is accompanied by concise discussions on their advantages and limitations.

A site-selective dual C-7 and C-6 C-H functionalization of indolines with azabenzonorbornadienes has been accomplished using Rh-catalysis. The reaction affords a potential route toward pyrrolocarbazoles with broad scope and functional group tolerance.

A simple, efficient and green procedure for the synthesis of novel 2,4-diaryl-5,6-dihydrobenzo[j][1,7]phenanthrolines has been developed via a Krohnke-type one-pot three-component reaction of 2-[arylmethylidene]-3,4-dihydro-1(2H)-acridinones and (2-aryl-2-oxoethyl)pyridinium bromides in the presence of excess ammonium acetate in good yields under solvent-free conditions. Good functional group tolerance, high substrate scope and no column purification are the practical advantages of this methodology.

Cobalt(ii)-catalyzed stereospecific coupling of N-methylanilines with styrene oxides is developed via tandem C-N and C-O bond formation using tert-butyl hydroperoxide (TBHP) as an oxidant. Optically active epoxide can be reacted with high optical purity.

An efficient one-pot microwave assisted stereoselective synthesis of novel dihydro-2'H-spiro[indene-2,1'-pyrrolo[3,4-c]pyrrole]-tetraone derivatives through three-component 1,3-dipolar cycloaddition of azomethine ylides generated in situ from ninhydrin and sarcosine with a series of 1-aryl-1H-pyrrole-2,5-diones is described. The synthesised compounds were screened for their antimycobacterial and AChE inhibition activities. Compound 4b (IC 50 1.30µM) has been found to display twelve fold antimycobacterial activity compared to cycloserine and it is thirty seven times more active than pyrimethamine. Compound 4h displays maximum AchE inhibitory activity with IC 50 value of 0.78±0.01µmol/L., (Copyright © 2017 Elsevier Ltd. All rights reserved.)

The combinatorial syntheses of a library of novel dihydrothiophenone-engrafted dispiro oxindole/indenoquinoxaline-pyrrolidine/pyrrolothiazole/indolizine hybrid heterocycles have been realized through a chemo-, regio-, and stereoselective multicomponent 1,3-dipolar cycloaddition strategy.

A facile stereoselective synthesis of novel dispiro indeno pyrrolidine/pyrrolothiazole-thiochroman hybrids has been achieved by 1,3-dipolar cycloaddition of azomethine ylides, generated in situ from ninhydrin and sarcosine/thiaproline, on a series of 3-benzylidenethiochroman-4-ones. The synthesised compounds were screened for their antimycobacterial, anticancer and AchE inhibition activities. Compound 4l (IC 50 1.07μM) has been found to exhibit the most potent antimycobacterial activity compared to cycloserine (12 times), pyrimethamine (37 times) and ethambutol (IC 50 <1.56μM) and 6l (IC 50 =2.87μM) is more active than both cycloserine (4 times) and pyrimethamine (12 times). Three compounds, 4a, 6b and 6i, display good anticancer activity against CCRF-CEM cell lines. Compounds 6g and 4g display maximum AchE inhibitory activity with IC 50 values of 1.10 and 1.16μmol/L respectively., (Copyright © 2016 Elsevier Ltd. All rights reserved.)

A library of novel dispiro compounds containing oxindole pyrrolidine/oxindolopyrrolothiazole-thiochroman-4-one hybrid frameworks has been synthesized in a fully regio- and stereoselective fashion by the three-component 1,3-dipolar cycloaddition of azomethine ylides generated in situ from the condensation of isatins and secondary amino acids (sarcosine/l-thioproline) with 3-arylidenethiochroman-4-ones. This experimentally simple protocol provides good yields of structurally complex, biologically relevant heterocycles in a single operation.

A novel protocol for the synthesis of 3-nitro-N-aryl/alkylthiophen-2-amines in good yields from the reaction of α-nitroketene N,S-aryl/alkylaminoacetals and 1,4-dithiane-2,5-diol in the presence of K2CO3 in refluxing ethanol is described. This transformation generates two C-C bonds in a single operation and presumably proceeds through a reaction sequence comprising 2-mercaptoacetaldehyde generation, nucleophilic carbonyl addition, annelation and elimination steps.

Herein, we report a metal-free, base-promoted route for the synthesis of hybrid molecular scaffolds in which various 1,3-diones and 1,2,4-triazoles are linked by a benzyl bridge. This three-component, one-pot reaction was accomplished by first treating 4-hydroxycoumarin, trans-β-nitrostyrene, and aldehyde hydrazone in the presence of sodium carbonate. Further, this protocol was successfully expanded to other 1,3-diones, such as dimedone and 4-hydroxy-2-quinolone. A broad substrate scope, mild reaction conditions, and the metal and ligand/additive-free approach are the prominent features of this strategy. [ABSTRACT FROM AUTHOR]

The 1,3-dipolar cycloaddition of azomethine ylides generated in situ from the reaction of isatins or acenaphthylene-1,2-dione and 1,3-thiazolane-4-carboxylic acid to various exocyclic dipolarophiles synthesized from estrone afforded a library of novel C-16 spiro oxindole or acenaphthylene-1-one - 7-(aryl)tetrahydro-1H-pyrrolo[1,2-c][1,3]thiazole - estrone hybrid heterocycles. These reactions occur regio- and stereo-selectively affording a single isomer of the spiro estrones in excellent yields with the formation of two C-C and one C-N bonds along with the generation of four new contiguous stereo-centers in a single step., (Copyright © 2014 Elsevier Inc. All rights reserved.)

C-H Functionalization is ubiquitously considered as a powerful, efficient and handy tool for installing various functional groups in complex organic heterocycles in an easier and step-economic way. Similarly, indazole is endowed as a potent heterocycle and is eminent for its profound impact in biological, medicinal and industrial chemistry. In this scenario, C-H functionalization at the selective ortho position of 2-arylindazole in assistance of a metal catalyst is also becoming an appealing approach in synthetic organic chemistry. This review addressed the recent findings and developments on ortho C-H functionalization of 2-aryl-2H-indazazoles with literature coverage extending from 2018 to May 2022., (© 2022 The Chemical Society of Japan & Wiley-VCH GmbH.)

Summary: Brain cancer is one of the leading diseases of death in the world caused due to unwanted proliferation of cells. If left untreated, this growth can spread into other human body parts. So early detection helps to enhance long‐term survival and reduce the mortality rate. A lot of research has been done in the field of brain tumors. There have been numerous previous studies conducted using traditional approaches. So far, few review studies are available on brain tumor segmentation and classification and moreover, they were quite limited in explaining the connections of Generative Adversarial Networks (GAN) for brain tumor segmentation and classification. This review mainly focuses on the GAN architectures for brain tumor segmentation and classification. Therefore, first, an overview of brain tumors, GAN‐based publications, approaches to brain tumor segmentation and classification, data sets, software platforms, and performance parameters, are presented. Finally, GAN applications and current trends are discussed. This thorough survey will aid researchers and beginners in the future in creating a better decision support system. [ABSTRACT FROM AUTHOR]

Comprehensive Summary: A thermally‐induced multi‐component reaction of CF3‐substituted imidoyl sulfoxonium ylides (TFISYs), amines and (triphenylphosphonio)difluoroacetate (PDFA) has been developed, allowing a facile access to 2‐trifluoromethyl‐4‐aminoquinolines in high yields. The reaction proceeds smoothly with or without the addition of sulfur and utilizes difluorocarbene as a C1 synthon under simply heating conditions. Mechanistic study reveals that in‐situ generated thiocarbonyl fluoride, isothiocyanate or gem‐difluoroalkene might act as the key reaction intermediates. [ABSTRACT FROM AUTHOR]

Looking for effective synthetic methods for 1H-pyrazolo[3,4-b]quinolines preparation, we came across a procedure where, in a three-component reaction catalysed by L-proline, 4-aryl-4,9-dihydro-1H-pyrazolo[3,4-b]quinolines are formed. These compounds can be easily oxidised to a fully aromatic system, which gives hope for a synthetic method that could replace, e.g., Friedländer condensation, often used for this purpose, even though severely limited by the availability of suitable substrates. However, after careful repetition of the procedures described in the publication, it turned out that the compounds described therein do not form at all. The actual compounds turned out to be 4,4-(phenyl-methylene)-bis-(3-methyl-1-phenylpyrazol-5-oles). Therefore, 4-Aryl-4,9-dihydro-1H-pyrazolo[3,4-b]quinolines were prepared by another method and used as standards to compare the products formed in the original procedure. [ABSTRACT FROM AUTHOR]

Green chemistry, which is an application of a set of principles to decrease or eliminate the use or creation of hazardous chemicals in the design, manufacture, and use of chemical commodities, is one of the most appealing concepts in chemistry for sustainability. Green chemistry has grown in popularity as a consequence of the understanding that environmentally friendly products and methods save mother nature over time. A fundamental key of synthetic chemistry is the creation of ecologically acceptable methods for the synthesis of organic molecules. In many biological applications, new molecules have been synthesized using environmentally friendly processes throughout the past few decades. It is also observed that, in the cycloaddition processes, nature-friendly approaches were focused significantly to avoid environmental pollution caused by toxic solvents and other additives. Hence, we as responsible chemists highly motivated to showcase the green synthetic methods adopted for cycloaddition reactions. In this study, we have reviewed nature-friendly methods utilized for the synthesis of new compounds via Diels–Alder and 1,3-dipolar cycloaddition reactions. [ABSTRACT FROM AUTHOR]

Enantiomerically enriched five‐ and six‐membered benzo oxygen heterocycles are privileged architectures in functional organic molecules. Over the last several years, many effective methods have been established to access these compounds. However, comprehensive documents cover updated methodologies still in highly demand. In this review, recent transition metal catalyzed transformations lead to chiral five‐ and six‐membered benzo oxygen heterocycles are presented. The mechanism and chirality transfer or control processes are also discussed in details. [ABSTRACT FROM AUTHOR]

Amino acids have a crucial role in the field of asymmetric organocatalysis for the production of chiral compounds with high added value and specific biological activity. In particular, proline offers high activity and stereoselectivity for catalyzing aldol reactions in organic solvents. However, proline-based catalysts often lack water-solubility, accessibility, catalytic performance, or recovery in aqueous media. This work reports the design of proline-functionalized poly(methyl methacrylate) (PMMA) nanoparticles with a magnetic core that offer high availability of chiral units in water and high recyclability. A proline-based copolymerizable surfactant is designed and integrated onto the surface of PMMA nanoparticles through a miniemulsion polymerization process without using additional surfactants. The miniemulsion technique allows the incorporation of magnetite to the system to create a magnetically separable catalyst. The chiral nanocatalyst presents a high diastereoselective catalytic activity for the intermolecular aldol reaction between p-nitrobenzaldehyde and cyclohexanone in water., (© 2024 The Author(s). Macromolecular Rapid Communications published by Wiley‐VCH GmbH.)

Development of environmentally benign catalyst systems, especially those derived from readily available nature's pool, in multicomponent synthesis, consolidates multiple facets of green chemistry. Here, an L-proline derived green acid catalyst in the form of L-proline⋅H 2 SO 4 was developed and employed for multicomponent synthesis of coumarin-based spiroindolino-3,4-dihydropyrimidin-2(1H)-ones from the reaction of 4-hydroxycoumarin, isatin and urea/thiourea. Preliminary cytotoxicity studies showed that a couple of compounds (M5 and M6) have good cytotoxicity (40-50%) against in Dalton's Lymphoma (DL) cells while demonstrating minimal cytotoxicity (10-12%) for normal non-cancerous cell lines. Molecular docking simulations for the least and most cytotoxic compounds, M3 and M6 respectively, against nineteen tumor target proteins were carried out, and seven of them were identified to test against all the sixteen compounds. Based on the estimated docking score and inhibition constants (K i ), the interaction of the compounds with the tumor target protein, beta-hexosaminidase B (PDB ID: 1NOW) matched closely with in vitro cytotoxicity data., (© 2024. The Author(s), under exclusive licence to Springer Nature Switzerland AG.)

The first example of asymmetric alkene–alkene reductive coupling is demonstrated via visible-light-fueled photoredox/cobalt dual catalysis. The desymmetrization reaction provided products (>20 examples) with up to five chiral centers in single-step operation in up to 95% yields with very high relative (>99 : 1 dr) and absolute stereochemistry (up to 98 : 2 er) control. The preliminary mechanistic investigations suggested that the critical mechanistic steps involved light-mediated controlled low-valent cobalt complex generation, oxidative ene–ene cyclization, and protonation. [ABSTRACT FROM AUTHOR]

The design and development of eco-friendly procedures for synthesizing organic compounds is an essential key to synthetic chemistry and has gained significant interest. The catalysts increase the rate of chemical reactions with additional advantages such as reduced energy input, diminished environmental impact, and overall financial benefit. The combined advantages of multicomponent reactions (MCRs) and natural catalysts will be an emerging and strategic area and is an ideal blend for the development of sustainable methodologies in organic synthesis. The plant, fruits, and their extracts and residues contain many useful chemical components lost during disposal. The crops contain renewable chemicals which are useful for catalysis and organic synthesis. Due to the excellent chemical properties of the natural extracts, they have gained great attention as cost-effective catalysts. In this review, we critically focus on using natural-based catalysts in multicomponent reactions that lead to synthetically and biologically relevant organic molecules and diverse heterocycles. The use of natural-based catalysts is cost-effective, favorable for work-up procedures, sustainable and industrial applications, and is usually more effective than traditional catalysts. [ABSTRACT FROM AUTHOR]

Rhodium‐catalyzed C−H activation has emerged as a powerful tool for forging C−C and C‐heteroatom bonds. Nevertheless, the requirement of stoichiometric chemical oxidants for oxidative transformations significantly hampered the overall sustainability of the C−H activation transformations. The emergence of merging transition metal catalysis and electrochemistry, called metalla‐electrocatalysis provides an excellent opportunity to construct organic molecules efficiently and sustainably. This review highlights the recent developments of rhodium‐catalyzed electrochemical C−H activation transformations, challenges and opportunities for future developments. [ABSTRACT FROM AUTHOR]

A Pd‐catalyzed enantioselective linear‐allylic alkylation of vinyl benzoxazinanones with a series of 3‐substituted oxindoles was reported in the presence of a chiral oxamide‐phosphine ligand (COAP−Bn) under mild reaction conditions. A series of optically active multifunctional 3,3′‐disubstituted oxindole derivatives bearing a quaternary stereogenic center and a linear aryl amino side chain were respectively obtained in 55–98% yields with 96–99% ee for 3‐(hetero)aryl substituted oxindoles. The developed protocol demonstrates that the COAP ligands could serve as a privileged chiral ligand to construct diverse chiral 3,3‐disubstituted oxindole compounds with various quaternary stereogenic centers, such as aza‐, thio‐ or all‐carbon quaternary stereogenic centers. The salient features of the method include broad substrate scope, N‐protecting group free, base‐free, and high regio‐ and enantioselectivity. [ABSTRACT FROM AUTHOR]

The oxidative [3+2+1] annulation reaction of aldehydes, 5‐aminopyrazoles, and nitriles is achieved under the oxidation of I2/O2, affording various valuable pyrazolo[3,4‐d]pyrimidines in 27%–91% yields. The salient feature of this reaction is transition‐metal free, operationally simple, broad substrate scope, good functional group tolerance, and gram‐scalable. Remarkably, the corresponding products exhibited intriguing photophysical properties such as Aggregation‐Induced Emission (AIE) and intramolecular charge transfer (ICT) and showed good potential to specifically light up lipid droplets (LDs) in living cells with bright fluorescence, low cytotoxicity, and good photostability. [ABSTRACT FROM AUTHOR]

Multicomponent reactions (MCRs) have emerged as a powerful strategy in synthetic organic chemistry due to their widespread applications in drug discovery and development. MCRs are flexible transformations in which three or more substrates react to form structurally complex products with high atomic efficiency. They are being increasingly appreciated as a highly exploratory and evolutionary tool by the medicinal chemistry community, opening the door to more sustainable, cost-effective and rapid synthesis of biologically active molecules. In recent years, MCR-based synthetic strategies have found extensive application in the field of drug discovery, and several anticancer drugs have been synthesized through MCRs. In this review, we present an overview of representative and recent literature examples documenting different approaches and applications of MCRs in the development of new anticancer drugs. [ABSTRACT FROM AUTHOR]

Synthesis of heterocyclic compounds is fundamental for all the research area in chemistry, from drug synthesis to material science. In this framework, catalysed synthetic methods are of great interest to effective reach such important building blocks. In this review, we will report on some selected examples from the last five years, of the major improvement in the field, focusing on the most important conventional catalytic systems, such as transition metals, organocatalysts, to more sustainable ones such as photocatalysts, iodine-catalysed reaction, electrochemical reactions and green innovative methods., (© 2023 The Authors. ChemSusChem published by Wiley-VCH GmbH.)

A four-component synthesis of 2-phenyl-9H-pyrimido[4,5-b]indoles was developed using indole-3-carboxaldehydes, aromatic aldehyde and ammonium iodide as the raw materials under transition-metal-free conditions. The pyrimidine ring was formed in one pot through [4 + 2] annulation reaction. Four C–N bonds were formed in one pot promoted by iodine and iodide additives. This work is highlighted by using two ammonium iodides as the sole nitrogen source. [ABSTRACT FROM AUTHOR]

(1) Background: The role of antihypertensives in Alzheimer's Disease (AD) prevention is controversial. This case-control study aims to assess whether antihypertensive medication has a protective role by studying its association with amyloid and tau abnormal levels. Furthermore, it suggests a holistic view of the involved pathways between renin-angiotensin drugs and the tau/amyloidß42 ratio (tau/Aß42 ratio); (2) Methods: The medical records of the participant patients were reviewed, with a focus on prescribed antihypertensive drugs and clinical variables, such as arterial blood pressure. The Anatomical Therapeutic Chemical classification was used to classify each drug. The patients were divided into two groups: patients with AD diagnosis (cases) and cognitively healthy patients (control); (3) Results: Age and high systolic blood pressure are associated with a higher risk of developing AD. In addition, combinations of angiotensin II receptor blockers are associated with a 30% lower t-tau/Aß42 ratio than plain angiotensin-converting enzyme inhibitor consumption; (4) Conclusions: Angiotensin II receptor blockers may play a potential role in neuroprotection and AD prevention. Likewise, several mechanisms, such as the PI3K/Akt/GSK3ß or the ACE1/AngII/AT1R axis, may link cardiovascular pathologies and AD presence, making its modulation a pivotal point in AD prevention. The present work highlights the central pathways in which antihypertensives may affect the presence of pathological amyloid and tau hyperphosphorylation. [ABSTRACT FROM AUTHOR]

N-fused pyrrolidinyl spirooxindole belongs to a class of privileged heterocyclic scaffolds and is prevalent in natural alkaloids and synthetic pharmaceutical molecules. To realize the switchable synthesis of divergent N-fused pyrrolidinyl spirooxindoles for further biological activity evaluation via a substrate-controlled strategy, a chemically sustainable, catalysis-free, and dipolarophile-controlled three-component 1,3-dipolar cycloaddition of isatin-derived azomethine ylides with diverse dipolarophiles is described in this work. A total of 40 functionalized N-fused pyrrolidinyl spirooxindoles were synthesized in 76–95% yields with excellent diastereoselectivities (up to >99:1 dr). The scaffolds of these products can be well-controlled by employing different 1,4-enedione derivatives as dipolarophiles in EtOH at room temperature. This study provides an efficient strategy to afford a spectrum of natural-like and potentially bioactive N-fused pyrrolidinyl spirooxindoles. [ABSTRACT FROM AUTHOR]

A Cu(I)‐catalyzed 1,3 oxo alkylation of indazole has been developed for constructing N‐1‐alkylated indazolone derivatives. This cascade reaction involves the formation of C−N and C−O bonds through the sequential functionalization of N1 and C3 positions of indazole in 41–89% yields. The photo‐physical studies of the synthesized compounds showed efficient quantum yields with high Stoke shift values. The preliminary experimental results suggest an aerobic manifold of the present protocol through single electron transfer. [ABSTRACT FROM AUTHOR]

Arylformylacetonitriles are versatile and attractive synthons in organic synthesis owing to their high reactivity. Among the numerous transformations involving arylformylacetonitriles, multicomponent reactions (MCRs) offer straightforward and effective routes to assemble the reactants into a wide range of five‐ and six‐membered heterocyclic systems including pyrrole, pyrazole, triazole, furan, pyridine, pyrimidine, and pyran. This review collects the recent advances and applications of arylformylacetonitriles in MCRs for the synthesis of monocyclic or polycyclic heterocycles published in the literature since 2001. [ABSTRACT FROM AUTHOR]

A synthetic route for the production of chiral derivatives of benzimidazole is presented. Different commercially available amines are evaluated as organocatalysts for the stereoselective aldol addition of N 1-benzimidazolyl acetaldehyde, previously prepared by N -alkylation of benzimidazole, with cyclic ketones. When cyclohexanone was used, l -prolinamide proved to be the most efficient catalyst, giving (S)-2-((R)-2-(1 H -benzo[ d ]imidazol-1-yl)-1-hydroxyethyl)cyclohexanone in 92% yield, 90% ee and 92:8 dr (anti / syn). [ABSTRACT FROM AUTHOR]

A one‐pot, three‐component protocol for the synthesis of 2‐aminothiazoles promoted by iodine from readily available starting materials such as β‐diketones/β‐ketoesters, arylamines, and NH4SCN has been developed. A wide range of arylamines was tolerated well to produce the expected polysubstituted 2‐aminothiazoles in moderate to good yields. The characteristic features of this methodology include operational ease, metal‐free reaction conditions, gram‐scale scalability, functional group tolerance, and short reaction times. [ABSTRACT FROM AUTHOR]

A regioselective Rh(III)-catalyzed C–H bond naphthylation and cascade directing group (DG) transformation has been realized with aryl imidates and oxa bicyclic alkenes. Diverse naphthalene-substituted aromatic esters were synthesized fruitfully. The DG transformation into ester endows the strategy with chances of further C–H bond functionalization and derivatization. Preliminary mechanistic studies demonstrate that the ester carbonyl oxygen possibly originates from the corresponding oxa bicyclic alkene. [ABSTRACT FROM AUTHOR]

An efficient access to a large array of diarylmethane thioether derivatives is developed through catalyst‐free 1,6‐conjugate addition of 1,4‐dithiane‐2,5‐diols with para‐quinone methides in high to excellent yields. Moreover, this reaction system is also suitable for other sulfur‐based nucleophiles, and the resulting products can be readily converted into other valuable diarylmethane derivatives. [ABSTRACT FROM AUTHOR]

C−H Functionalization is ubiquitously considered as a powerful, efficient and handy tool for installing various functional groups in complex organic heterocycles in an easier and step‐economic way. Similarly, indazole is endowed as a potent heterocycle and is eminent for its profound impact in biological, medicinal and industrial chemistry. In this scenario, C−H functionalization at the selective ortho position of 2‐arylindazole in assistance of a metal catalyst is also becoming an appealing approach in synthetic organic chemistry. This review addressed the recent findings and developments on ortho C−H functionalization of 2‐aryl‐2H‐indazazoles with literature coverage extending from 2018 to May 2022. [ABSTRACT FROM AUTHOR]

The 1,3-dipolar cycloaddition reaction is a three-component reaction used for the synthesis of structurally complex and biologically active spiro-heterocycles. In the present work a two steps synthesis of the target compounds (7-22) are presented. 2-acetyl phenothiazine was converted into a chalcone 1 which was treated with various azomethine ylides to yield the compounds 7-22. The diversity in the azomethine ylides was made by using a variety of diones 2a-2d and the different aminoacids 3-6. The anti-cancer activity of the compounds 7-22 was evaluated by testing against breast cancer MCF-7 cell lines by MTT assay. Compounds 7, 12, 16 and 20 exhibited potent anticancer activity against MCF-7 breast cancer cell lines with an IC50 values of 83.08, 84.68, 95.68 and 114.23 µg/mL respectively and non toxic towards normal fibroblast L929 cells. In the Cell cycle analysis of compound 7 arrests the cell cycle in MCF-7 cells. [ABSTRACT FROM AUTHOR]

A catalyst‐free protocol for synthesizing a new series of indeno[1,2‐b][1,6]naphthyridine‐1,10(2H)‐dione derivatives with good to excellent yields was established based on microwave‐assisted domino reaction of 4‐aminopyridin‐2(1H)‐ones, aldehydes and 1H‐indene‐1,3(2H)‐dione in water. The present approach exhibited useful and green features, such as water as reaction solvent, catalyst‐ and additive‐ free, short reaction time (20–30 min), as well as ease of desired products separation and purification without the need for column chromatography. Also to note, up to four new bonds were formed accompanied by generating water as sole by‐product in this one‐pot procedure. [ABSTRACT FROM AUTHOR]

A strategy for catalyst-free domino reaction of 4-aminopyridin-2(1H)-ones, arylglyoxal hydrates and different 1,3-dicarbonyl compounds in water has been established. The mild and efficient procedure afforded pyrrolo[3,2-c]pyridine derivatives with 76–94% yields after simple crystallization. The present procedure shows promising characteristics, such as readily available starting materials, the use of water as reaction media, simple and efficient one-pot operation, and avoiding the need for any hazardous or expensive catalysts. [ABSTRACT FROM AUTHOR]