(2S,4E)-5-氯-2-异丙基-4-戊烯酸乙酯的简易合成  

Concise Synthesis of Ethyl(2S,4E)-5-choro-2-isopropylpent-4-ene carboxylate

作　　者：吴桂平[1] 王有名[1] 周正洪[1] 

机构地区：[1]南开大学元素有机化学国家重点实验室元素有机化学研究所,天津300071

出　　处：《精细化工中间体》2012年第4期40-41,53,共3页Fine Chemical Intermediates

摘　　要：以异戊酸乙酯与(E)-1,3-二氯丙烯为原料,通过烷基化反应得到(±)-(4E)-5-氯-2-异丙基-4-戊烯酸乙酯,经猪肝酯酶催化(进行动力学拆分)得到纯阿利克仑(Aliskiren)中间体(2S,4E)-5-氯-2-异丙基-4-戊烯酸乙酯。通过回收拆分母液以88%的收率得到(2R,4E)-5-氯-2-异丙基-4-戊烯酸。该方法绿色环保,操作简洁易行,具有工业化应用前景。Ethyl(±)-(4E)-5-choro-2-isopropylpent-4-ene carboxylate was synthesized from ethyl isovalerate and(E)-1,3-dichloropropene,followed by conversion to ethyl(2S,4E)-5-choro-2-isopropylpent-4-ene carboxylate,a key intermediate for Aliskiren,by porcine liver esterase catalyzed dynamic kinetic resolution(DKR).At the mean time,(2R,4E)-5-chloro-2-(1-methylethyl)-4-pentenoic acid was obtained in 88% yield by recycling the mother liquid.In summary,an environmentally friendly practical method has been developed.

关 键 词：阿利克 1 3-(E)-1 3-二氯丙烯 猪肝酯酶 (2S 4E)-5-氯-2-异丙基-4-戊烯酸乙酯 动力学拆分 

分 类 号：TQ463+.54[化学工程—制药化工]