Open AccessJournal Article
Expedient protocol for the installation of thiadiazole on 2-position of 1,4-benzodiazepin-5-carboxamide through a phenoxyl spacer
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TL;DR: An efficient single step strategy for the heteroannulation of 2-chloro-1,4benzodiazepine ring, substituted in its 5position with a carboxamido group, has been developed to allow the easy installation of thiadiazole (8) ring through thiosemicarbazone (7) intermediate as discussed by the authors.
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Abstract: An efficient novel single step strategy for the heteroannulation of 2-chloro-1,4benzodiazepine ring, substituted in its 5-position with a carboxamido group (5), has been developed to allow the easy installation of thiadiazole (8) ring through thiosemicarbazone (7) intermediate. In this communication, exceedingly facile single step expedient protocols based on the versatility and reactivity of corresponding intermediate thiosemicarbazone (7), derived from 5-carboxamido-1,4-benzodiazepin-5(4’-methylpiperazinyl)-carboxamide (5) have been developed to provide an easy installation of the thiadiazole (8) privileged template at 2-position of 5-carboxamido-1,4benzodiazepin-5-(4’-methylpiperazinyl)-carboxamide, through a phenoxyl spacer.
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A facile one pot synthesis of novel pyrimidine derivatives of 1,5-benzodiazepines via domino reaction and their antibacterial evaluation
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Eric B. Lansdon,Katherine M. Brendza,Magdeleine Hung,Ruth Wang,Susmith Mukund,Debi Jin,Gabriel Birkus,Nilima Kutty,Xiaohong Liu +8 more
TL;DR: Crystal structures were determined with wild-type and K103N HIV-1 reverse transcriptase with etravirine and rilpivirine, revealing a similar binding mode for TMC125 and TMC278, whether bound to wild- type or K103n RT.
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1,5-Benzothiazepine, a versatile pharmacophore: a review.
Jitender Bariwal,Kuldip Upadhyay,Atul Manvar,Jalpa C. Trivedi,Jyoti Singh,Kishor S. Jain,Anamik Shah +6 more
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