摘要
以异丁酰乙酸甲酯为原料经苯胺胺解得到4-甲基-3-氧-N-苯戊酰胺,然后与苯甲醛发生反应,得到4-甲基-3-氧-N-苯-2-(苯亚甲基)戊酰胺,再以溴化噻唑为催化剂,与对氟苯甲醛发生Stetter反应,得到阿托伐他汀钙的关键中间体4-(4-氟苯基)-2-(2-甲基丙酰基)-4-氧代-N,β-二苯基丁酰胺.该方法操作简便,收率较高,各主要化合物结构经核磁共振氢谱确证.
4-（4-Fluorophenyl）-2-（2-methylpropanoyl）-4-oxo-N,β-diphenylbutanamide is a key intermediate of atorvastatin.Methyl isobutyryl acetate was transformed into 4-methyl-3-oxo-N-pentanamide by reaction with aniline;the resulting product could undergo Knoevenagel condensation with benzaldehyde giving 4-mehtyl-3-oxo-N-Phenyl-2-（Phenylmethylene）Pentanamide,which could further undergo Stetter reation with p-fluorobenzaldehyde thus giving aceess to the final molecule 4-（4-Fluorophenyl）-2（2-methylpropanoyl）-4-oxo-N,β-diphenylbutanamide.The synthetic route were easily available and the yield was reasonable.The structures of the main intermediates were identified by 1H NMR.
出处
《武汉工程大学学报》
CAS
2010年第12期10-12,共3页
Journal of Wuhan Institute of Technology
