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In recent years, Despite the proven economic growth brought by AI technology globally, the adoption of AI in the construction industry faces obstacles. To better promote the adoption of AI technology in the construction domain, this study, based on the extended Unified Theory of Acceptance and Use of Technology (UTAUT) model, delves into the key factors influencing the adoption of AI technology in the construction industry. By introducing personal-level influencing factors such as AI anxiety and personal innovativeness, the UTAUT model is extended to comprehensively understand users’ attitudes and adoption behaviors towards AI technology.The research framework is based on the Unified Theory of Acceptance and Use of Technology (UTAUT) with the added constructs of artificial intelligence anxiety and individual Innovativeness. These data were collected through a combination of online and offline surveys, with a total of 258 valid data collected and analyzed using structural equation modeling.The study found that Usage Behavior (UB) in adopting Artificial Intelligence (AI) is positively influenced by several factors. Specifically, Performance Expectancy (PE) (β= 0.266, 95%), Effort Expectancy (EE) (β= 0.262, 95%), and Social Influence (SI) (β= 0.131, 95%) were identified as significant predictors of UB. Additionally, Facilitating Conditions (FC) (β= 0.168, 95%) also positively influenced UB.Moreover, the study explored the moderating effects of Artificial Intelligence Anxiety and Individual Innovativeness on the relationships between Performance Expectancy (PE), Effort Expectancy (EE), Social Influence (SI), and Facilitating Conditions (FC) with the Usage Behavior of AI technology.This study lie in informing industry stakeholders about the multifaceted dynamics influencing AI adoption. Armed with this knowledge, organizations can make informed decisions, implement effective interventions, and navigate the challenges associated with integrating AI technology into the construction sector. [ABSTRACT FROM AUTHOR]

Synthetic cannabinoid receptor agonists (SCRAs) remain a major public health concern, with their use implicated in intoxications and drug-related deaths worldwide. Increasing our systematic understanding of SCRA metabolism supports clinical and forensic toxicology casework, facilitating the timely identification of analytical targets for toxicological screening procedures and confirmatory analysis. This is particularly important as new SCRAs continue to emerge on the illicit drug market. In this work, the metabolism of ADB-HEXINACA (ADB-HINACA, N -[1-amino-3,3-dimethyl-1-oxobutan-2-yl]-1-hexyl-1 H -indazole-3-carboxamide), which has increased in prevalence in the United Kingdom and other jurisdictions, was investigated using in vitro techniques. The (S)-enantiomer of ADB-HEXINACA was incubated with pooled human hepatocytes over 3 hours to identify unique and abundant metabolites using liquid chromatography–quadrupole time-of-flight mass spectrometry. In total, 16 metabolites were identified, resulting from mono-hydroxylation, di-hydroxylation, ketone formation (mono-hydroxylation then dehydrogenation), carboxylic acid formation, terminal amide hydrolysis, dihydrodiol formation, glucuronidation and combinations thereof. The majority of metabolism took place on the hexyl tail, forming ketone and mono-hydroxylated products. The major metabolite was the 5-oxo-hexyl product (M9), while the most significant mono-hydroxylation product was the 4-hydroxy-hexyl product (M8), both of which were confirmed by comparison to in-house synthesized reference standards. The 5-hydroxy-hexyl (M6) and 6-hydroxy-hexyl (M7) metabolites were not chromatographically resolved, and the 5-hydroxy-hexyl product was the second largest mono-hydroxylated metabolite. The structures of the terminal amide hydrolysis products without (M16, third largest metabolite) and with the 5-positioned ketone (M13) were also confirmed by comparison to synthesized reference standards, along with the 4-oxo-hexyl metabolite (M11). The 5-oxo-hexyl and 4-hydroxy-hexyl metabolites are suggested as biomarkers for ADB-HEXINACA consumption. [ABSTRACT FROM AUTHOR]

Rilmazafone is a pro-drug that can be prescribed in Japan to treat insomnia. Rilmazafone metabolizes into active compounds by a ring closure resulting in a triazolo benzodiazepine structure similar to alprazolam. In mid-2022, the National Board of Forensic Medicine in Sweden were requested to investigate two separate deaths with the suspected use of pagoclone. Packages labeled "Pagoclone" were found at each scene that was suspected to contain rilmazafone based on website information. During screening by high resolution mass spectrometry, rilmazafone metabolites were presumptively identified. Due to the lack of reference material for the active metabolites, the metabolites were synthesized in house and quantification of the compounds identified in the two autopsy cases was prompted. In Case 1, femoral blood concentrations of 7.9, 65 and 170 ng/g of the metabolites rilmazolam, N -desmethyl rilmazolam and di-desmethyl rilmazolam, respectively, were detected. Additional toxicological findings included the medications haloperidol, alimemazine, fluoxetine, olanzapine and acetaminophen. In Case 2, femoral blood concentrations of 1.7, 1.4 and 70 ng/g of rimazolam, N -desmethyl rilmazolam and di-desmethyl rilmazolam, respectively, were detected. Additional toxicological findings included loperamide, alimemazine and pregabalin. The intake of rilmazafone was determined as the cause of death in Case 1 and contributed in the Case 2. [ABSTRACT FROM AUTHOR]

Acetylbenzylfentanyl, benzoylbenzylfentanyl, 3‐fluoro‐methoxyacetylfentanyl, and 3‐phenylpropanoylfentanyl are fentanyl analogs that have been reported to the European Monitoring Centre for Drugs and Drug Addiction in recent years. The aim of this study was to identify metabolic pathways and potential biomarker metabolites of these fentanyl analogs. The compounds were incubated (5 μM) with cryopreserved hepatocytes for up to 5 h in vitro. Metabolites were analyzed with liquid chromatography–quadrupole time of flight–high‐resolution mass spectrometry (LC‐QTOF‐HRMS). The experiments showed that acetylbenzylfentanyl, benzoylbenzylfentanyl, and 3‐phenylpropanoylfentanyl were mainly metabolized through N‐dealkylation (forming nor‐metabolites) and 3‐fluoro‐methoxyacetylfentanyl mainly through demethylation. Other observed metabolites were formed by mono‐/dihydroxylation, dihydrodiol formation, demethylation, dehydrogenation, amide hydrolysis, and/or glucuronidation. The experiments showed that a large number of metabolites of 3‐phenylpropanoylfentanyl were formed. The exact position of hydroxy groups in formed monohydroxy metabolites could not be established solely based upon recorded MSMS spectra of hepatocyte samples. Therefore, potential monohydroxy metabolites of 3‐phenylpropanoylfentanyl, with the hydroxy group in different positions, were synthesized and analyzed together with the hepatocyte samples. This approach could reveal that the β position of the phenylpropanoyl moiety was highly favored; β‐OH‐phenylpropanoylfentanyl was the most abundant metabolite after the nor‐metabolite. Both metabolites have the potential to serve as biomarkers for 3‐phenylpropanoylfentanyl. The nor‐metabolites of acetylbenzylfentanyl, benzoylbenzylfentanyl, and 3‐fluoro‐methoxyacetylfentanyl do also seem to be suitable biomarker metabolites, as do the demethylated metabolite of 3‐fluoro‐methoxyacetylfentanyl. Identified metabolic pathways and formed metabolites were in agreement with findings in previous studies of similar fentanyl analogs. [ABSTRACT FROM AUTHOR]

Early warning systems detect new psychoactive substances (NPS), while dedicated monitoring programs and routine drug and toxicology testing identify fluctuations in prevalence. We report the increasing prevalence of the synthetic cannabinoid receptor agonist (SCRA) ADB‐BUTINACA (N‐[1‐amino‐3,3‐dimethyl‐1‐oxobutan‐2‐yl]‐1‐butyl‐1H‐indazole‐3‐carbox‐amide). ADB‐BUTINACA was first detected in a seizure in Sweden in 2019, and we report its detection in 13 routine Swedish forensic toxicology cases soon after. In January 2021, ADB‐BUTINACA was detected in SCRA‐infused papers seized in Scottish prisons and has rapidly increased in prevalence, being detected in 60.4% of the SCRA‐infused papers tested between January and July 2021. In this work, ADB‐BUTINACA was incubated with human hepatocytes (HHeps), and 21 metabolites were identified in vitro, 14 being detected in authentic case samples. The parent drug and metabolites B9 (mono‐hydroxylation on the n‐butyl tail) and B16 (mono‐hydroxylation on the indazole ring) are recommended biomarkers in blood, while metabolites B4 (dihydrodiol formation on the indazole core), B9, and B16 are suitable biomarkers in urine. ADB‐4en‐PINACA (N‐[1‐amino‐3,3‐dimethyl‐1‐oxobutan‐2‐yl]‐1‐[pent‐4‐en‐1‐yl]‐1H‐indazole‐3‐carboxamide) was detected in Scottish prisons in December 2020, but, unlike ADB‐BUTINACA, prevalence has remained low. ADB‐4en‐PINACA was incubated with HHeps, and 11 metabolites were identified. Metabolites E3 (dihydrodiol formed in the tail moiety) and E7 (hydroxylation on the linked/head group) are the most abundant metabolites in vitro and are suggested as urinary biomarkers. The in vitro potencies of ADB‐BUTINACA (EC50, 11.5 nM and ADB‐4en‐PINACA (EC50, 11.6 nM) are similar to that of MDMB‐4en‐PINACA (EC50, 4.3 nM). A third tert‐leucinamide SCRA, ADB‐HEXINACA was also detected in prison samples and warrants further investigation. [ABSTRACT FROM AUTHOR]

Fentanyl analogues have appeared on the recreational drug market during the last ten years and caused many fatal overdoses around the world due to their high potencies. Their metabolites are of great interest for toxicology, metabolism and identification studies. According to the literature, fentanyl analogues with similar structures have similar metabolism profile. Therefore, a synthetic route that enables synthesis of the corresponding metabolites for several fentanyl analogues would be valuable. Fentanyl analogue metabolites are often polar and tailing on silica gel. Hence, the purification of these substances could be challengeable. In this work, a general synthetic route was developed and described for the multi-gram scale synthesis of 14 potential metabolites of seven fentanyl analogues. The synthetic route is concise and optimized, does not require any use of silica gel purification and is therefore convenient for large-scale synthesis. The overall yields of the metabolites were in the range of 25–57%. [ABSTRACT FROM AUTHOR]

Objective: About one third of all patients with epilepsy have pharmacoresistant seizures. Thus there is a need for better pharmacological treatments. The human voltage‐gated potassium (hKV) channel hKV7.2/7.3 is a validated antiseizure target for compounds that activate this channel. In a previous study we have shown that resin acid derivatives can activate the hKV7.2/7.3 channel. In this study we investigated if these channel activators have the potential to be developed into a new type of antiseizure drug. Thus we examined their structure‐activity relationships and the site of action on the hKV7.2/7.3 channel, if they have unwanted cardiac and cardiovascular effects, and their potential antiseizure effect. Methods: Ion channels were expressed in Xenopus oocytes or mammalian cell lines and explored with two‐electrode voltage‐clamp or automated patch‐clamp techniques. Unwanted vascular side effects were investigated with isometric tension recordings. Antiseizure activity was studied in an electrophysiological zebrafish‐larvae model. Results: Fourteen resin acid derivatives were tested on hKV7.2/7.3. The most efficient channel activators were halogenated and had a permanently negatively charged sulfonyl group. The compounds did not bind to the sites of other hKV7.2/7.3 channel activators, retigabine, or ICA‐069673. Instead, they interacted with the most extracellular gating charge of the S4 voltage‐sensing helix, and the effects are consistent with an electrostatic mechanism. The compounds altered the voltage dependence of hKV7.4, but in contrast to retigabine, there were no effects on the maximum conductance. Consistent with these data, the compounds had less smooth muscle–relaxing effect than retigabine. The compounds had almost no effect on the voltage dependence of hKV11.1, hNaV1.5, or hCaV1.2, or on the amplitude of hKV11.1. Finally, several resin acid derivatives had clear antiseizure effects in a zebrafish‐larvae model. Significance: The described resin acid derivatives hold promise for new antiseizure medications, with reduced risk for adverse effects compared with retigabine. [ABSTRACT FROM AUTHOR]

Synthetic cannabinoid metabolites with a 5F-4OH pentyl side chain are of great interest, and several synthetic methods have been developed for the synthesis of these types of metabolites in the literature, which is either lengthy or inappropriate for upscaling. Herein, a straightforward method has been developed and reported for the synthesis of a key intermediate in four steps with an overall yield of 49% on a multigram scale, and its application in the synthesis of nine potential metabolites of synthetic cannabinoids with a 5F-4OH pentyl side chain. [ABSTRACT FROM AUTHOR]

Fentanyl analogs constitute a particularly dangerous group of new psychoactive compounds responsible for many deaths around the world. Little is known about their metabolism, and studies utilizing liquid chromatography–quadrupole time-of-flight mass spectrometry (LC–QTOF-MS) analysis of hepatocyte incubations and/or authentic urine samples do not allow for determination of the exact metabolite structures, especially when it comes to hydroxylated metabolites. In this study, seven motifs (2-, 3-, 4- and β-OH as well as 3,4-diOH, 4-OH-3-OMe and 3-OH-4-OMe) of fentanyl and five fentanyl analogs, acetylfentanyl, acrylfentanyl, cyclopropylfentanyl, isobutyrylfentanyl and 4F-isobutyrylfentanyl were synthesized. The reference standards were analyzed by LC–QTOF-MS, which enabled identification of the major metabolites formed in hepatocyte incubations of the studied fentanyls. By comparison with our previous data sets, major urinary metabolites could tentatively be identified. For all analogs, β-OH, 4-OH and 4-OH-3-OMe were identified after hepatocyte incubation. β-OH was the major hydroxylated metabolite for all studied fentanyls, except for acetylfentanyl where 4-OH was more abundant. However, the ratio 4-OH/β-OH was higher in urine samples than in hepatocyte incubations for all studied fentanyls. Also, 3-OH-4-OMe was not detected in any hepatocyte samples, indicating a clear preference for the 4-OH-3-OMe, which was also found to be more abundant in urine compared to hepatocytes. The patterns appear to be consistent across all studied fentanyls and could serve as a starting point in the development of methods and synthesis of reference standards of novel fentanyl analogs where nothing is known about the metabolism. [ABSTRACT FROM AUTHOR]

MMB022 (methyl 3‐methyl‐2‐[1‐(pent‐4‐en‐1‐yl)‐1H‐indole‐3‐carboxamido]butanoate) is a new synthetic cannabinoid with an alkene at the pentenyl side chain, a rare functional group for synthetic cannabinoids. Metabolite identification is an important step for the detection of synthetic cannabinoids in humans, since they are generally extensively metabolized. The aims of the study were to tentatively identify in vitro phase I metabolites, to confirm major metabolites using synthesized metabolites, to examine metabolic pathways thoroughly, to study metabolic stability and to suggest metabolites appropriate for urine screening. MMB022 and its synthesized metabolites were incubated with human liver microsomes (HLM) and the supernatants were analyzed by liquid chromatography‐quadrupole time‐of‐flight mass spectrometry. Sixteen metabolites were identified, which were generated via dehydrogenation, dihydrodiol formation, ester hydrolysis, hydroxylation, and combinations thereof. A major biotransformation of the alkene at the pentenyl side chain was confirmed to be dihydrodiol formation. The major metabolites were ester hydrolysis (M15) and dihydrodiol (M8) metabolites, whereas the metabolite derived from the combination of ester hydrolysis and dihydrodiol (M5) was the fourth most abundant metabolite. The metabolic pathways were investigated using synthesized metabolites and revealed that M5 is an end product of the pathways, indicating that it might become a more abundant metabolite in vivo depending on the rate of metabolism in humans. The major pathway of MMB022 to M5 was determined to be via M8 formation. Intrinsic clearance of MMB022 was determined to be 296 mL/min/kg and t1/2 was 2.1 min, indicating a low metabolic stability. M15, M8, and potentially M5 are suggested as suitable urinary targets. [ABSTRACT FROM AUTHOR]

Synthetic cannabinoids are a group of compounds that act on the CB1 receptor and are used illicitly as substitutes for cannabis. Given the rapid and extensive metabolism of synthetic cannabinoids, urinary biomarkers are essential if proof of drug intake is to be obtained in forensic laboratories. To identify good biomarker candidates, the metabolism of synthetic cannabinoids must be studied and reference standards need to be acquired. Studies on the metabolism of synthetic cannabinoids containing a terminally fluorinated pentyl side chain have shown that hydroxylation can occur at the four position of the side chain. This makes the 4-hydroxy-5-fluoropentyl side-chain metabolite a good urinary biomarker for proving intake of the corresponding parent drug, as this compound cannot be formed from its nonfluorinated analogue. Here, a concise synthetic route to the 4-hydroxy-5-fluoropentyl side-chain metabolites of the synthetic cannabinoids STS-135, MAM-2201, AM-2201, and XLR-11 is reported. [ABSTRACT FROM AUTHOR]

Cyclopropylfentanyl is a fentanyl analog implicated in 78 deaths in Europe and over 100 deaths in the United States, but toxicological information including metabolism data about this drug is scarce. The aim of this study was to provide the exact structure of abundant and unique metabolites of cyclopropylfentanyl along with synthesis routes. In this study, metabolites were identified in 13 post-mortem urine samples using liquid chromatography quadrupole time-of-flight mass spectrometry (LC-QTOF-MS). Samples were analyzed with and without enzymatic hydrolysis, and seven potential metabolites were synthesized in-house to provide the identity of major metabolites. Cyclopropylfentanyl was detected in all samples, and the most abundant metabolite was norcyclopropylfentanyl (M1) that was detected in 12 out of 13 samples. Reference materials were synthesized (synthesis routes provided) to identify the exact structure of the major metabolites 4-hydroxyphenethyl cyclopropylfentanyl (M8), 3,4-dihydroxyphenethyl cyclopropylfentanyl (M5) and 4-hydroxy-3-methoxyphenethyl cyclopropylfentanyl (M9). These metabolites are suitable urinary markers of cyclopropylfentanyl intake as they are unique and detected in a majority of hydrolyzed urine samples. Minor metabolites included two quinone metabolites (M6 and M7), not previously reported for fentanyl analogs. Interestingly, with the exception of norcyclopropylfentanyl (M1), the metabolites appeared to be between 40% and 90% conjugated in urine. In total, 11 metabolites of cyclopropylfentanyl were identified, including most metabolites previously reported after hepatocyte incubation. [ABSTRACT FROM AUTHOR]

We revisited the Congo red analogue 2,5‐bis(4′‐hydroxy‐3′‐carboxy‐styryl)benzene (X‐34) to develop this highly fluorescent amyloid dye for imaging Alzheimer's disease (AD) pathology comprising Aβ and Tau fibrils. A selection of ligands with distinct optical properties were synthesized by replacing the central benzene unit of X‐34, with other heterocyclic moieties. Full photophysical characterization was performed, including recording absorbance and fluorescence spectra, Stokes shift, quantum yield and fluorescence lifetimes. All ligands displayed high affinity towards recombinant amyloid fibrils of Aβ1‐42 (13–300 nm Kd) and Tau (16–200 nm Kd) as well as selectivity towards the corresponding disease‐associated protein aggregates in AD tissue. We observed that these ligands efficiently displaced X‐34, but not Pittsburgh compound B (PiB) from recombinant Aβ1‐42 amyloid fibrils, arguing for retained targeting of the Congo red type binding site. We foresee that the X‐34 scaffold offers the possibility to develop novel high‐affinity ligands for Aβ pathology found in human AD brain in a different mode compared with PiB, potentially recognizing different polymorphs of Aβ fibrils. [ABSTRACT FROM AUTHOR]

A Suzuki–Miyaura coupling reaction of ortho‐hydroxyaromatic bromide 8 with isopropenylboronic acid pinacol ester has been investigated. It was found that the catalyst of Pd2(dba)3/PCy3 in dioxan‐water gave good yield by suppressing the formation of isomeric side product 14. (+)‐Callitrisic acid was synthesized from (+)‐podocarpic acid using this condition with an overall yield of 54 % in about five steps. (+)‐Callitrisic acid was found to be almost three times more potent than dehydroabietic acid to open a voltage‐gated potassium channel. [ABSTRACT FROM AUTHOR]

25C-NBOMe and 25I-NBOMe are potent hallucinogenic drugs that recently emerged as new psychoactive substances. To date, a few metabolism studies were conducted for 25I-NBOMe, whereas 25C-NBOMe metabolism data are scarce. Therefore, we investigated the metabolic profile of these compounds in human hepatocytes, an in vivo mouse model and authentic human urine samples from forensic cases. Cryopreserved human hepatocytes were incubated for 3 h with 10 μM 25C-NBOMe and 25I-NBOMe; samples were analyzed by liquid chromatography high-resolution mass spectrometry (LC-HRMS) on an Accucore C18 column with a Thermo QExactive; data analysis was performed with Compound Discoverer software (Thermo Scientific). Mice were administered 1.0 mg drug/kg body weight intraperitoneally, urine was collected for 24 h and analyzed (with or without hydrolysis) by LC-HRMS on an Acquity HSS T3 column with an Agilent 6550 QTOF; data were analyzed manually and with WebMetabase software (Molecular Discovery). Human urine samples were analyzed similarly. In vitro and in vivo results matched well. 25C-NBOMe and 25I-NBOMe were predominantly metabolized by O-demethylation, followed by O-di-demethylation and hydroxylation. All methoxy groups could be demethylated; hydroxylation preferably occurred at the NBOMe ring. Phase I metabolites were extensively conjugated in human urine with glucuronic acid and sulfate. Based on these data and a comparison with synthesized reference standards for potential metabolites, specific and abundant 25C-NBOMe urine targets are 5'-desmethyl 25C-NBOMe, 25C-NBOMe and 5-hydroxy 25C-NBOMe, and for 25I-NBOMe 2' and 5'-desmethyl 25I-NBOMe and hydroxy 25I-NBOMe. These data will help clinical and forensic laboratories to develop analytical methods and to interpret results. Copyright © 2016 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]

In this work, emergence patterns of synthetic cannabinoids were utilized in an attempt to predict those that may appear on the drug market in the future. Based on this information, two base structures of the synthetic cannabinoid analogues - (1 H-indol-3-yl(2,2,3,3-tetramethylcyclopropyl)methanone and 1 H-indol-3-yl(adamantan-1-yl)methanone) - together with three substituents - butyl, 4-fluorobutyl and ethyl tetrahydropyran - were selected for synthesis. This resulted in a total of six synthetic cannabinoid analogues that to the authors' knowledge have not yet appeared on the drug market. Spectroscopic data, including nuclear magnetic resonance (NMR), mass spectrometry (MS), and Fourier transform infrared (FTIR) spectroscopy (solid and gas phase), are presented for the synthesized analogues and some additional related cannabinoids. In this context, the suitability of the employed techniques for the identification of unknowns is discussed and the use of GC-FTIR as a secondary complementary technique to GC-MS is addressed. Examples of compounds that are difficult to differentiate by their mass spectra, but can be distinguished based upon their gas phase FTIR spectra are presented. Conversely, structural homologues where mass spectra are more powerful than gas phase FTIR spectra for unambiguous assignments are also exemplified. This work further emphasizes that a combination of several techniques is the key to success in structural elucidations. Copyright © 2015 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]

In an effort to identify a new class of druglike HIV-1proteaseinhibitors, four different stereopure β-hydroxy γ-lactam-containinginhibitors have been synthesized, biologically evaluated, and cocrystallized.The impact of the tether length of the central spacer (two or threecarbons) was also investigated. A compound with a shorter tether and(3R,4S) absolute configuration exhibitedhigh activity with a Kiof 2.1 nM andan EC50of 0.64 μM. Further optimization by decorationof the P1′ side chain furnished an even more potent HIV-1 proteaseinhibitor (Ki= 0.8 nM, EC50= 0.04 μM). According to X-ray analysis, the new class ofinhibitors did not fully succeed in forming two symmetric hydrogenbonds to the catalytic aspartates. The crystal structures of the complexesfurther explain the difference in potency between the shorter inhibitors(two-carbon spacer) and the longer inhibitors (three-carbon spacer). [ABSTRACT FROM AUTHOR]

A para substitution pattern of the phenyl ring is a characteristicfeature of the first reported selective AT2receptor agonistM024/C21 (1) and all the nonpeptidic AT2receptoragonists described so far. Two series of compounds structurally relatedto 1but with a meta substitution pattern have now beensynthesized and biologically evaluated for their affinity to the AT1and AT2receptors. A high AT2/AT1receptor selectivity was obtained with all 41 compounds synthesized,and the majority exhibited Kirangingfrom 2 to 100 nM. Five compounds were evaluated for their functionalactivity at the AT2receptor, applying a neurite outgrowthassay in NG108-15 cells. Notably, four of the five compounds, withrepresentatives from both series, acted as potent AT2receptorantagonists. These compounds were found to be considerably more effectivethan PD 123,319, the standard AT2receptor antagonist usedin most laboratories. No AT2receptor antagonists werepreviously reported among the derivatives with a para substitutionpattern. Hence, by a minor modification of the agonist 1it could be transformed into the antagonist, compound 38. These compounds should serve as valuable tools in the assessmentof the role of the AT2receptor in more complex physiologicalmodels. [ABSTRACT FROM AUTHOR]

Abstract: A fast and efficient microwave promoted one-pot method for deoxygenation of heterocyclic halo-benzyl alcohols has been developed. The method does not cause dehalogenation of the substrates and provides the deoxygenated products in high yield after only 30min. [Copyright &y& Elsevier]

A mild and efficient method for deprotection of tert-butyl sulfonamide groups utilizing Sc(OTf)3 as deprotecting reagent has been developed. A variety of tert-butyl aryl sulfonamides used under these conditions gave the corresponding primary sulfonamides in high yields. The Lewis acid catalyst could be fully recovered and reused with maintained activity after the reactions. [ABSTRACT FROM AUTHOR]

A fast method utilizing in situ generated CO for the synthesis of phthalides has been developed. DMF and Mo(CO)6 were applied as two alternative CO-sources in these microwave promoted carbonylation–lactone formation reactions. Mo(CO)6 was found to be the more generally applicable CO-source and provided phthalides as well as dihydroisocoumarin, dihydroisoindone, and phthalimide from the corresponding aryl bromide via an efficient CO insertion within a 1 h reaction time. [Copyright &y& Elsevier]