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Abstract: Quinoline and pyrimidine are well-known moieties, which appear in various natural and synthetic products. Furthermore, quinoline-pyrimidine-inspired hybrids are known to have several biological properties. In addition, many pyrimido[4,5-b]quinolinone ring systems, specifically concerning medicinal chemistry, have been reported over the past decade. This review depicts the synthesis of pyrimido[4, 5-b] quinolones (PyQs4,5-b) through 6-aminopyrimidin-4-(thi)one derivatives. The preparation of PyQs4,5-b was clarified through the following chemical reactions: Vilsmeier-Haack formylation, Hantzsch-like reaction, and one-pot three-component reaction.

Abstract: This review described the preparation of 2-chloroquinoline-3-carbaldehyde derivatives through Vilsmeier-Haack formylation of N-arylacetamides and the use of them as a key intermediate for the preparation of 2-aminoquinoline-3-carbaldehydes. The synthesis of the 2-aminoquinolines was explained through the following chemical reactions: Claisen-Schmidt condensation, 1, 3-dipolar cycloaddition, one-pot multicomponent reactions (MCRs), and reductive amination.

Abstract: Quinoline ring system is extensively dispensed in natural products, especially in alkaloids. Moreover, thieno[2,3-b]quinolines have vast biological activities, including urea transporter inhibition, anti-microbial, antitumor, antioxidant, anti-inflammatory, and antiproliferative EGFR tyrosine kinase inhibition. Vilsmeier-Haack is considered the most facile and promising set of synthetic routes, leading to 2-chloro-3-formylquinolines through Vilsmeier-Haack cyclisation of N- arylacetamides, which are subsequently used as key intermediates for the synthesis of thieno[2,3-b]quinolones (Tqs). Many varieties of thieno[2,3-b]quinolines (Tqs) ring systems, specifically concerning medicinal chemistry, have been developed over the past decade. In light of these facts, this review presents a systematic and comprehensive survey of the method of preparation and the chemical reactivity of thieno[2,3-b]quinolines through the Vilsmeier-Haack reaction. In this study, the methods of preparation and the chemical reactivity of (Tqs) by using the Vilsmeier-Haack reaction are discussed. Since the beginning of the 21st century, they have been advancing towards synthesizing substituted Tqs. It can be concluded that substituted Tqs can be used as building blocks for the synthesis of polyfunctionalized heterocyclic compounds with pharmacological interest.

Background: Vilsmeier-Haack formylation of N-arylacetamides and used them as a key intermediate for preparation of 2-(piperidin-1-yl) and/ or 2-(morpholin-1-yl) quinoline-3- carbaldehydes. these used as precursors for the synthesis of 2-(piperidin-1-yl) and/ or 2-(morpholin- 1-yl) quinoline derivatives through the reaction with active methyl and/ or methylene component, Claisen-Schmidt condensation, one-pot multicomponent reactions (MCRs), reductive amination, Grignard reaction, etc. Methods: This review demonstrates the synthesis of 2-chloroquinoline-3-carbaldehyde derivatives, through Vilsmeier-Haack formylation of N-arylacetamides that used as a precursor for preparation of 2-(piperidin-1-yl) and/ or 2-(morpholin-1-yl) quinoline- 3-carbaldehydes and reacted them with various reagents to form the 2-(piperidin-1-yl) and/ or 2-(morpholin-1-yl) quinolines derivatives. Results: Many 2-(piperidin-1-yl) and/ or 2-(morpholin-1-yl) quinolines derivatives were achived through the reaction with active methyl and/ or methylene component, Claisen-Schmidt condensation, one-pot multicomponent reactions (MCRs), reductive amination, Grignard reaction, etc…. Conclusion: Many quinoline ring systems, specifically concerning medicinal chemistry, had been published over the past decade. During this review, we have outlined the synthetic routes and reactions of 2-(piperidin-1-yl) and/ or 2-(morpholin-1-yl) quinoline-3-carbaldehydes. This review implies a section of the synthesis of 2-(piperidin-1-yl) and/ or 2-(morpholin-1-yl) quinoline-3-carbaldehydes which can be prepared via Vilsmeier formylation of N-arylacetamides followed by heating of the formed aldehydes with piperidine or morpholine and two sections on its reactions with different reagents were presented. Eventually, this review focus upon 2-(piperidin-1-yl) and/ or 2-(morpholin-1- yl) quinoline-3-carbaldehydes as an interesting heterocyclic compound that can be utilized as a precursor and building block for the synthesis of an extended range of heterocyclic systems which have a potent pharmacological interest.

Abstract: The biological and medicinal properties of thieno[3, 2-c] quinoline have prompted enormous research aimed at developing synthetic routes for these systems. This review focuses on the chemical properties associated with this system. The most reported reactions are Bischler- Napieralski, Suzuki−Miyaura−Schlüter, Pictet-Spengler, Stille coupling and Friedlander and Beckmann rearrangement reaction.

Abstract: The improvement of new synthetic routes towards thiophene, oxazole, triazole, pyrimidine, pyridine, quinolone, coumarin, imidazopyrimidine, pyridoimidazole and triazolo[1,5-a] pyridine for their biological and medicinal exploration is an appealing vicinity for researchers. This review focuses on the utility of 1-(4-substituted-aminophenyl) ethanones and their derivatives as critical intermediates for the synthesis of these systems developed within the closing decade.

Abstract: Several thieno [2,3-h] /[3,2-h] quinolines and thieno [2,3-f] /[3,2-f] quinolines (TQs) are discussed in this review from a few perspectives, including various preparation and processing methods employing cutting-edge machinery. The preparation of (TQs), from 4-(5)aminobenzothiophene, 2(3)chloromethylthiophene, 2(3)thienylboric acid, and other chemical reagents is illustrated via a number of chemical procedures in this review. The formation of (TQs) was clarified using the Michael addition, Photocyclization, Skraup reaction, Ullmann-Fetvadjian process, Suzuki-Miyaura and Sonogashira reaction, aza-Diels-Alder reaction, and Friedel-Crafts reaction.

Abstract: This review described the preparation of 2- chloroquinoline-3-carbaldehyde derivatives 18 through Vilsmeier-Haack formylation of N-arylacetamides and the use of them as a key intermediate for the preparation of 2-(piperazin-1-yl) quinoline-3-carbaldehydes. The synthesis of the 2- (piperazin-1-yl) quinolines derivatives was explained through the following chemical reactions: acylation, sulfonylation, Claisen-Schmidt condensation, 1, 3-dipolar cycloaddition, one-pot multicomponent reactions (MCRs), reductive amination, Grignard reaction and Kabachnik-Field’s reaction.

Abstract: This review describes the synthesis and chemical reactivity of tetrahydrothieno[3,2-b] quinoline derivatives from through many of the reagents such as; 1, 2-dihydropyridine-3-carbonitrile; 1,6-dihydropyrimidine-5-carbonitrile; 2,3-dihydropyridazine-4-carbonitrile; 3-amino-thiophene-2-carboxylate; 3-amino-thiophene-2-carbonitrile; 3,4-diaminothieno[2,3-b] thiophene-2,5-dicarbo- nitrile; 2-(3-bromo-1-iodoisoquinolin-8-yl) benzonitrile and 3-mercapto-benzo[g]quinolin-4(1H)-one derivatives. The synthesis of the tetrahydrothieno [3, 2-b] quinoline derivatives were explained through the following chemical reactions: Aldol condensation, alkylation, cyclocondensation, dehydration, chlorination, Wolff-Kishner reduction, acylation, Friedlander reaction and intramolecular cyclization.

Abstract: In this review, numerous thieno[2,3-c]quinoline derivatives (TQs2, 3-c) are presented from a variety of angles, including various preparation and processing techniques, using cutting-edge equipment. Numerous chemical processes in this review demonstrate how (TQs2, 3-c) were made from arylamines, ketones, aldehydes, carboxylic acids, and other chemical reagents. The amidation, tandem C-C and C-N bond creation accelerated by palladium, Vilsmeier reaction, and Pictet-Spengler chemical reactions were used to shed light on how (TQs2, 3-c) was made.

Abstract: In this review article, many thieno[2,3-c]quinoline derivatives are shown from many aspects, including different preparation and processing methods, by the use of recent systems and high technology. This review includes many chemical reactions that show the preparation of thieno[2,3-c]quinoline derivatives from arylaldehyde, arylamine derivatives, and other chemical reagents.

Pyrazolone and its derivatives are an crucial class of heterocyclic compounds that may be traced in in a number of well-established drugs, such as celecoxib, Lonazolac and Mepirizole (anti-inflamma...

Abstract: 4H-Pyran is a well-known moiety, which appears in various natural and synthetic products. These compounds include various biological activities like anti-hepatotoxic, antitumor, anti-inflammatory, antioxidant, anti-spasmolytic, diuretic, estrogenic, anticoagulant, antifungal, antiviral, anti-helminthic, antimicrobial, hypothermal, anti-tubercular, anti-HIV, herbicidal, anticonvulsant and analgesic activity. This review has summarized an overview of general strategies that allow the design of 4H-pyran derivatives via catalyzed one-pot multicomponent reactions.

This review describes the synthesis and reactions of substituted triazolopyrimidines as building blocks toward polyfunctionalized heterocyclic compounds with pharmacological interest.

Novel chitosan nanoparticles (SCN) were synthesized via reaction of chitosan with different concentration of 2-chloro-N-(3-methylisoxazol-5-yl) acetamide (5 %, 10 % and 15 %) at 70–80 °C for 7 h to give the grafted polymer, which condensed with cyclohexanone Mannich base 45 °C for 7 h to afford the corresponding (SCN). These were stirred with Deflazacort drug to achieve the Deflazacort loading (SCN), which, compressed with calcium starch glycolate (CaSgly) to give the corresponding tablets. The pH 2. 1 and concentration of SCN-10 %/CaSgly (1:4) was found to be important parameters in controlling the release profiles.

The biological, therapeutic, and medicinal properties of fused 1, 3, 4-thiadiazines, 1, 3, 5-thiadiazines, 1, 2, 4-thiadiazines, and 1, 2, 6-thiadiazines, and their analogues have prompted enormous...

This review highlights the development of an efficient and practically different catalyst for organic transformation to synthesize valuable 1(5)-substituted 1H-tetrazoles and their analogs.

Damping-off, root rot and necrotic lesions were observed on sugar beet (Beta vulgaris) seedlings in the Kafrelsheikh Governorate, in the northern part of the Nile River delta, Egypt. Pythium aphanidermatum was identified as the causal agent using the morphology of the asexual and sexual morphs and molecular studies. This is the first record of P. aphanidermatum on sugar beet in Egypt.

This review describes the synthesis and reactions of substituted pyrazolo[3,4-b] pyridines as a building block for the synthesis of polyfunctionalized heterocyclic compounds with pharmacological interest.

This review presents a systematic and comprehensive survey of the chemical reactivity of 3-acyl(aroyl) coumarins. The target compounds are important intermediates for the synthesis of a variety of synthetically useful and novel heterocyclic systems with different ring sizes such as isoxazole, pyrazole, 3H-triazolium salts, pyrimidine, pyridine, quinolone, benzoxocin, benzoxonin and benzoxepin. &nbsp

The development of new synthetic routes towards pyrazolo[1,5-a]pyrimidines for their biological and medicinal exploration is an attractive area for researchers. This review focuses on various synthetic routes developed in the last decade for the synthesis of differently substituted pyrazolo[1,5-a]pyrimidines by a broad range of organic reactions by means of 5-aminopyrazole as a precursor.

Novel Chitosan-cyclohexanone Mannich based hydrogel nanoparticles (CCMb1-4) were prepare via the reaction of chitosan with different concentration of 2, 6-bis (piperidin-1-ylmethyl) cyclohexanone. ...

BACKGROUND phthalazine derivatives were reported to possess anticonvulsant , cardiotonic , antibacterial, analgesic , anti-inflammatory, and anti-microbial activity. In the current study, we applied the QSAR for prediction of newly phthalazinediones incorporating thioamide moiety aiming to reach a more potent anti-inflammatory and Analgesic agent. METHODS Phthalazinediones 10-15 have been synthesized through condensation of dibenzobarallene 3 with thiosemicarbazides 4-8. One equation was predicted using quantitative structure activity relationship (QSAR) and regression analysis for the anti-inflammatory activity with a regression correlation (R) close to unity. The docking studies were performed to investigate the biological trends of the organic compounds (thiol form) against cyclooxygenas- 2 enzyme, which is a responsible inflammation mediator by using Molgro Virtual Docker (MVD) software. The anti-inflammatory activity and analgesic effect of the thioamides 10-15 were determined by collagen II-adjuvant induced paw edema test in rats. RESULTS Compounds 10, 11, 12, and 14, exhibited promising anti-inflammatory activity. Furthermore, in the pain scoring, compounds 10, 11 and 12 were found to be more effective than piroxicam and the order of the analgesic effect of the investigated compounds is as followed 14 >12 > 10 > 11 > 15. CONCLUSION It is clear from the foregoing that the compound 14 is a promising compound if future pharmacological detailed studies. This is consistent with what has been predictable equation 1 in this study.

In this study, we present the synthesis of novel isothiochromenes, thiazolidonone, thiazinone, arylidines, triazoles, and pyrimidinone compounds based on the starting material 3-amino- isothiochromene-4-carbonitrile 3. The chemical structures were confirmed using spectroscopic methods and elemental analyses. These compounds were screened for their in vitro antiviral and antitumor activities. Compounds 10a-c and 22a-b showed activity against herpes simplex virus-1 (HSV-1) and human immunodeficiency virus-1 (HIV-1). Compounds 15 and 21a-b exhibited activity against various types of cancer cell lines.

Coumarins units have recently emerged as a hot topic of research due to their diverse applications. Their synthesis is partly based on classical methodologies such as Pechmann reaction or Knoevenag...

Novel biodegradable pH and thermal-responsive hydrogels were prepared for controlled drug delivery studies via reaction of chitosan with 4-chloroacetylantipyrine in DMF/H2O, followed by heating of ...

The biological and medicinal properties of nicotinonitrile and its analogues have prompted enormous research aimed at developing synthetic routes to these heterocyclic. This review highlights the d...