Solid-Phase Synthesis of 4,7,8-Trisubstituted 1,2,3,4-Tetrahydro-benzo[e][1,4]diazepin-5-ones

被引：7

作者：

Lemrova, Barbora ^{[1
]}

Soural, Miroslav ^{[1
]}

机构：

[1] Palacky Univ, Fac Sci, Inst Mol & Translat Med, Dept Organ Chem, Olomouc 77146, Czech Republic

来源：

ACS COMBINATORIAL SCIENCE | 2012年 / 14卷 / 12期

关键词：

benzodiazepinones; benzodiazocinones; thiazines; thiazepines; bisheterocycles; solid-phase synthesis; INHIBITORS; DESIGN; 5H-1,4-BENZODIAZEPIN-5-ONES;

D O I：

10.1021/co300121d

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Solid-phase synthesis of 1,2,3,4-tetrahydro-benzo[e][1,4]diazepin-S-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 add 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.

引用

页码：645 / 650

页数：6

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