Integrated Ugi-based assembly of functionally, skeletally, and stereochemically diverse 1,4-benzodiazepin-2-ones.

J Org Chem

Centro Singular de Investigación en Quı́mica Biológica y Materiales Moleculares (CIQUS) and ‡Departamento de Quı́mica Orgánica, Facultad de Farmacia, Universidad de Santiago de Compostela , E-15782 Santiago de Compostela, Spain.

Published: February 2015

A practical, integrated and versatile U-4CR-based assembly of 1,4-benzodiazepin-2-ones exhibiting functionally, skeletally, and stereochemically diverse substitution patterns is described. By virtue of its convergence, atom economy, and bond-forming efficiency, the methodology documented herein exemplifies the reconciliation of structural complexity and experimental simplicity in the context of medicinal chemistry projects.

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Source
http://dx.doi.org/10.1021/jo502382qDOI Listing

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