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Synfacts 2011(10): 1147-1147  
DOI: 10.1055/s-0030-1261086
Polymer-Supported Synthesis
© Georg Thieme Verlag Stuttgart ˙ New York

Solid-Phase Synthesis of Tetrahydrobenzo-diazepine Derivatives

Contributor(s): Yasuhiro Uozumi, Yoichi M. A. Yamada, Takuma Sato
Z. Liu, W. Chen, M. A. Giulianotti, R. A. Houghten*
Torrey Pines Institute for Molecular Studies, Port St. Lucie, USA
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Publication History

Publication Date:
20 September 2011 (online)

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Significance

A solid-phase synthesis of 2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepines, the core structure of drug scaffolds, was described. Starting from p-methylbenzhydrylamino resin (MBHA resin) and 2-nitrobenzoic acids, the desired benzodiazepines were obtained in 62-78% overall yield in seven steps (12 examples).