阿立哌唑的合成  

Synthesis of aripiprazole

作　　者：朱航昌[1] 陈国华[1] 张军忍[1] 李强[1] 

机构地区：[1]中国药科大学药物化学教研室,江苏南京210009

出　　处：《中国药物化学杂志》2006年第2期108-109,共2页Chinese Journal of Medicinal Chemistry

摘　　要：以间氨基苯甲醚为原料,经缩合、傅克酰化、成醚、取代4步制得抗精神病药阿立哌唑,并对原工艺进行改进。目标物的化学结构经红外光谱、核磁共振氢谱及质谱确证,该合成方法原料易得,操作简便,总收率为45·1%。Aripiprazole was synthesized by condensation of 7- （4-bromobutoxy）-3, 4-dihydrocarbostyril （5） and 1-（2, 3-dichlorolphenyl）-piperazine dihydrochloride. Compound 5 was prepared by condensation of 7- hydroxy-3, 4-dihydrocarbostyril（4） and 1,4-dibromobutane. Compound 4 was obtained from m-anisidine by condensation and F-C acylation. The structure of target compound was confirmed by IR,^1H-NMR, MS and the total yield was 45.1%. This procedure has advantages of simple starting material and convenient operations.

关 键 词：药物化学 药物制备 工艺改进 阿立哌唑 

分 类 号：R914.5[医药卫生—药物化学]