7-氯-5-氧代-2,3,4,5-四氢-1H-1-苯并氮杂的合成  

Synthesis of 7-Chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine

作　　者：杨妙[1] 帅军[2] 刘默[3] 刘登科[3] 王平保[3] 

机构地区：[1]天津医科大学,天津300070 [2]天津大学,天津300072 [3]天津药物研究院,天津300193

出　　处：《中国医药工业杂志》2009年第9期648-650,共3页Chinese Journal of Pharmaceuticals

基　　金：“重大新药创制”科技重大专项项日(2009ZX09103-078);天津市科技计划项目(09ZCKFSH01300)

摘　　要：5-氯-2-硝基苯甲酸经酯化、还原得到2-氨基-5-氯苯甲酸甲酯,然后经磺酰化、N-烷基化、Dieckmann缩合,再经脱羧、脱磺酸基保护得到V_2受体拮抗剂托伐普坦的关键中间体7-氯-5-氧代-2,3,4,5-四氢-1H-1-苯并氮杂,总收率约37%。7-Chloro-5-oxo-2,3,4,5-tetrahydro-lH-1-benzazepine, the key intermediate of V2 receptor antagonist tolvaptan was synthesized from 5-chloro-2-nitrobenzoic acid by esterification and reduction to give methyl 2-amino- 5-chlorobenzoate, which was subjected to sulfonylation, N-alkylation and Dieckmann condensation, followed by decarboxylation and deprotection with an overall yield of about 3 7 %.

关 键 词：7-氯-5-氧代-2 3 4 5-四氢-1H-1-苯并氮杂 托伐普坦 中间体 合成 

分 类 号：O626.5[理学—有机化学]