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
收藏
页码：645 / 650
页数：6
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