Solid-Phase Synthesis of 4,7,8-Trisubstituted 1,2,3,4-Tetrahydro-benzo[e][1,4]diazepin-5-ones
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- 作者：Barbora Lemrov谩 ; Miroslav Soural
- 刊名：ACS Combinatorial Science
- 出版年：2012
- 出版时间：December 10, 2012
- 年：2012
- 卷：14
- 期：12
- 页码：645-650
- 全文大小：370K
- 年卷期：v.14,no.12(December 10, 2012)
- ISSN：2156-8944
文摘
Solid-phase synthesis of 1,2,3,4-tetrahydro-benzo[e][1,4]diazepin-5-ones with use of polystyrene resin is described. The starting material was polymer supported 1,2-diaminoethane and as a key synthon, 4-chloro-2-fluoro-5-nitrobenzoic acid was used. The synthetic approach allows the preparation of derivatives with variable substitution at positions 4 and 8. Additionally, a skeletal diversity was increased when the nitro group was reduced and some benzene fused heterocycles were prepared. An expansion of a diazepinone to a benzodiazocinone scaffold was also successful although some limitations in a diversity of target derivatives were observed.