Soluble polymer-supported synthesis of benzodiazepinones

Cheng Yi Wu, Chung-Ming Sun*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

6 Scopus citations

Abstract

Soluble polymer-supported synthetic method provides a highly efficient route for the construction of biologically important 1,5-benzodiazepin-2-ones. A library of N-substituted benzodiazepinones can be readily assembled utilizing SNAr reaction, reduction of nitro group and one-pot cyclization following N-alkylation as the key step in the synthesis. All reactions in the sequence were performed at room temperature to facilitate the generation of libraries in a parallel fashion. The crude products were obtained in 80-95% yield with 60-96% HPLC purity.

Original languageEnglish
Pages (from-to)959-962
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume12
Issue number6
DOIs
StatePublished - 25 Mar 2002

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