首页> 外文期刊>Organic Preparations and Procedures International: The New Journal for Organic Synthesis >Preparation of 5,10,11,11a-tetrahydro-1H,3H-thiazolo2,3-c-and 5,10,11,11a-tetrahydro-1H,3H-thiazolo4,3-c-1,4benzodiazepines
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Preparation of 5,10,11,11a-tetrahydro-1H,3H-thiazolo2,3-c-and 5,10,11,11a-tetrahydro-1H,3H-thiazolo4,3-c-1,4benzodiazepines

机译:Preparation of 5,10,11,11a-tetrahydro-1H,3H-thiazolo2,3-c-and 5,10,11,11a-tetrahydro-1H,3H-thiazolo4,3-c-1,4benzodiazepines

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摘要

Benzodiazepines are perceived as "privileged" heterocyclic scaffolds for the genesis of drug candidates because this subunit tends to confer interesting biological activity to molecules.~(1-7) For example, benzodiazepines are important components of anxiolytics,~1 vasopressin receptor antagonists,~2,3 non-opioid analgesics,~4 and cholecystokinin receptor antagonists.~5 Additionally, pyrrolo[1,4] benzodiazepine antibiotics have attracted attention as potent anticancer agents.~6 Although the syntheses of a variety of benzodiazepines are well cocumented, preparations of heterocyclic systems 4 and 7 are unknown. Since we needed intermediates 4 and 7 for a medicinal chemistry project, we developed convenient synthetic methods, which are reported herein.

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