摘要
2-氯-4-硝基苯甲酸经酯化、水合肼还原所得4-氨基-2-氯苯甲酸甲酯,与5-氟-2-甲基苯甲酰氯经酰化、水解及酰氯化反应制得2-氯-4-[(5-氟-2-甲基苯甲酰基)氨基]苯甲酰氯,再与10,11-二氢-5H-吡咯并[2,1-c][1,4]苯并二氮反应制得选择性精氨酸加压素V2受体拮抗剂利希普坦,总收率约57%(以2-氯-4-硝基苯甲酸计)。
Lixivaptan, a selective arginine vasopressin V2 receptor antagonist, was synthesized from 2-chloro-4- nitrobenzoic acid by esterification, reduction with hydrazine hydrate, acylation with 5-fluoro-2-methylbenzoyl chloride, hydrolysis and acyl chlorination to give 2-chloro-4-[ （5-fluoro-2-methylbenzoyl）amino] benzoyl chloride, which was subjected to reaction with 10,11-dihydro-5H-pyrrolo [2,1-c] [1,4] benzodiazepine with an overall yield of about 57 % （based on 2-chloro-4-nitrobenzoic acid）.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2013年第12期1201-1204,共4页
Chinese Journal of Pharmaceuticals
基金
国家"重大新药创制"科技重大专项(2013ZX09102-014
2011ZX09401-009)
