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Synthesis of novel benzo[b]pyrazolo[1,5]diazepines

✍ Scribed by Joseph Raker; Yi Wang; Anthony D. Pechulis; James C. Haber; Michael A. Lynch; Stacey L. Spring

Publisher
Journal of Heterocyclic Chemistry
Year
2011
Tongue
English
Weight
125 KB
Volume
49
Category
Article
ISSN
0022-152X

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✦ Synopsis

Abstract

The synthesis and in vitro biological evaluation of two novel benzodiazepine derivatives are described. The compounds were synthesized divergently from the key amino alcohol 5, which was realized using the unusual Weinreb‐enamino ketone 10. J. Heterocyclic Chem., (2012).

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A facile approach to pyrazolo [4,3-e][1,4] diazepin-5,8-diones andpyrazolo[4,3-e]pyrrolo[1,2-a][1,4]diazepin-5,10-diones is reported. Strategy involved the utility of Ξ±-amino acid as a three-atom segment in the construction of diazepine skeleton on the preformed pyrazole ring.