两步法合成(S)-1-(2-氯乙酰基)-2-腈基吡咯烷的工艺研究  

Technology of two-step synthesis for (S)-1-(2-chloroacetyl)pyrrolidine-2-carbonitrile

作　　者：朱莹[1] 李玲[2] 赵世明[2] 罗振福[2] 孙波[1] 

机构地区：[1]天津理工大学化学化工学院,天津300384 [2]天津药物研究院化学制药部,天津300193

出　　处：《现代药物与临床》2013年第4期491-493,共3页Drugs & Clinic

摘　　要：目的研究(S)-1-(2-氯乙酰基)-2-腈基吡咯烷的合成工艺。方法 L-脯氨酸与氯乙酰氯通过N-乙酰化得到(S)-1-(2-氯乙酰基)-2-吡咯烷甲酸,然后加入脲素和氨基磺酸实行分段保温反应得到产物(S)-1-(2-氯乙酰基)-2-腈基吡咯烷。结果此路线所得产品收率为75.5%。结论此工艺路线条件温和、操作简便、原料价廉易得。Objective To study the synthesis of （S）-1-（2-chloroacetyl）pyrrolidine-2-carbonitrile. Methods L-Proline was N-acylated with chloroacetyl chloride to prepare （S）-1-（2-chloroacetyl）pyrrolidine-2-carboxylic acid, then urea and sulfamic acid were added, and （S）-1-（2-chloroacetyl）pyrrolidine-2-carbonitrile was given by using segmented insulation. Results The yield of （S）-1-（2-chloroacetyl） pyrrolidine-2-carbonitrile was 75.5%. Conclusion The reaction conditions of this route are mild, operation is easy, and the materials are common and inexpensive.

关 键 词：(S)-1-(2-氯乙酰基)-2-腈基吡咯烷 维格列汀 分段保温 

分 类 号：R914[医药卫生—药物化学]