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Communication
A Novel Strategy for the Construction of Functionalized 1,5- Benzodiazepines via a Tandem Conjugated Addition/Cyclization Process
Article first published online: 27 JAN 2010
DOI: 10.1002/adsc.200900736
Copyright © 2010 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Additional Information
How to Cite
Li, J., Li, S., Li, C., Liu, Y. and Jia, X. (2010), A Novel Strategy for the Construction of Functionalized 1,5- Benzodiazepines via a Tandem Conjugated Addition/Cyclization Process. Adv. Synth. Catal., 352: 336–340. doi: 10.1002/adsc.200900736
Publication History
- Issue published online: 17 FEB 2010
- Article first published online: 27 JAN 2010
- Manuscript Revised: 3 DEC 2009
- Manuscript Received: 22 OCT 2009
Funded by
- National Natural Science Foundation of China. Grant Numbers: 20872087, 20902057
- Key Laboratory of Synthetic Chemistry of Natural Substances
- Chinese Academy of Sciences
- Leading Academic Discipline Project of Shanghai Municipal Education Commission. Grant Number: J50101
- Innovation Fund of Shanghai University
Keywords:
- 1,5-benzodiazepines;
- conjugated addition;
- cyclization;
- tandem reactions
Abstract
A novel approach for the synthesis of functionalized 1,5-benzodiazepine is described. The protocol is triggered by a tandem conjugated addition/cyclization process from the readily available starting materials 1,2-phenylenediamine and ethyl propiolate. The products have secondary amino and ester groups, and a β-enamino ester, which can serve in further functionalizations to produce molecular diversity.