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.
出处
《中国药物化学杂志》
CAS
CSCD
2006年第2期108-109,共2页
Chinese Journal of Medicinal Chemistry
关键词
药物化学
药物制备
工艺改进
阿立哌唑
medicinal chemistry
drug preparation
process improvement
aripiprazole
