(S)-1-(1-苯基乙基)-4-哌啶酮的合成  

Synthesis of (S)-1-(1-Phenylethyl)-4-piperidone

作　　者：王娟[1] 李美玲[1] 陈立功[2] 李阳[2] 闫喜龙[2] 王东华[1] 

机构地区：[1]天津大学药物科学与技术学院,天津300072 [2]天津大学化工学院,天津300072

出　　处：《精细化工》2007年第11期1109-1111,共3页Fine Chemicals

摘　　要：该文以(S)-1-苯乙胺、丙烯酸甲酯为原料,经Michael加成,Dieckmann环合,脱羧,合成了(S)-1-(1-苯基乙基)-4-哌啶酮。并对所涉及的Michael加成反应的工艺参数进行了优化。当(S)-1-苯乙胺与丙烯酸甲酯的摩尔比为1∶2.5,40℃反应10h,收率为92.4%,总收率为89.3%。目标产物及中间体的结构经核磁共振波谱进行了表征。（S） -1-（1-Phenylethyl） -4-piperidone（ I ） was prepared from （S） -1-phenylethylamine and methyl acrylate through Michael addition, Dieckmann cyclization and decarboxylation. Technological parameters involved in Michael addition were optimized. Thus, （S） -1-phenylethylamine reacted with methyl acrylate in mole ratio 1：2.5 under 40 ℃ for 10 h to give the intermediate in 92.4% yield, and the total yield of I was 89.3%. Structures of the title compound and the intermediate were confirmed by ^1HNMR and ^13CNMR.

关 键 词：哌啶酮 MICHAEL加成 Dieckmann环合 脱羧 药物中间体 

分 类 号：TQ460.31[化学工程—制药化工]