Benzothiazepine, a prominent “drug prejudice core”, is a heterocyclic moiety of immense importance due to its presence in a wide range of bioactive compounds. They act as a primary “biolinker” in diverse synthetic routes to obtain bioactive molecules and serve as important templates in synthetic and medicinal chemistry. They are known to possess a plethora of pharmacological activities, which include Ca2+ channel blockers, CNS acting agents, anti‐HIV, ACE inhibitors, antimicrobial, antifungal, anticancer. Their promising behaviour as drug molecules led the scientific community to develop novel, mild, green, and highly efficient synthetic routes for their synthesis. The conventional synthesis generally involved the condensation of chalcones with 2‐aminothiophenol in the presence of acid/base with high‐temperature heating, mostly resulting in poor yields or mixtures. However, recent trends are replacing these conditions with mild and green conditions through organocatalysis or other methodologies. In this review, an attempt has been made by authors to summarize (a) Recent developments in the synthetic strategies of 1,5‐benzoathiazepines and its derivatives (b) Conventional methods for the synthesis of 1,5‐benzothiazepines including progress in the green chemistry routes (c) Applications of various metals and organocatalysts to achieve the enantioselective synthesis of title compounds.
The ubiquitous presence of 4-quinolones and its derivatives in a wide range of natural as well as synthetic drug molecules made them molecule of utmost importance for organic and medicinal chemists. Their wide array of biological activities such as antimicrobial, anticancer, anti-HIV, genitourinary infection, antifilarial, etc., has augmented their appeal both for synthetic and medicinal chemistry campaigns. Moreover, they are valuable intermediates for the synthesis of various fused heterocyclic compounds of synthetic and medicinal importance. Considering their array of synthetic and biological importance, new strategies for the synthesis of 4-quinolones and their derivatives have been designed and successfully demonstrated by researchers around the globe. The present review covers recent advances in the synthetic chemistry of 4quinolones since 2015 along with an insight into their mechanistic studies. We hope that the review article will serve as a valuable tool for the scientific community engaged in the synthesis and utilization of 4-quinolones and their derivatives.
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