(S)-1-苯基-1,2,3,4-四氢异喹啉的合成工艺改进  

Synthetic(S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline

作　　者：孔祥雨 杨利 张彬 李新志 崔新强 刘文涛 张宁 王洪臣 KONG Xiang-yu;YANG li;ZHANG Bin;LI Xin-zhi;CUI Xin-qiang;LIU Wen-tao;ZHANG Ning;WANG Hong-chen(Shandong Academy of Pharmaceutical Science,Key Lab for Chemical Drug Research of Shandong Province,Jinan 250101,China;Shandong Haiyou Freda Pharmaceutical Co.,Ltd”Linyi 276700,China)

机构地区：[1]山东省药学科学院山东省化学药物重点实验室,山东济南250101 [2]山东海佑福瑞达制药有限公司,山东临沭276700

出　　处：《精细化工中间体》2020年第1期44-47,共4页Fine Chemical Intermediates

摘　　要：以苯乙胺为起始原料,经苯甲酰化、脱水环合、还原,然后经酒石酸拆分得到(S)-1-苯基-1,2,3,4-四氢异喹啉,优化条件下,产品总收率76.3%,产品纯度99.5%,其结构经熔点、~1H NMR、MS确证。工艺操作简单,无特殊设备要求,适合工业化生产。(S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline was prepared through a series of reactions including benzoylation,dehydration cyclization,reduction and resolution with D-tartaric acid using phenylethylamine as a starting material.The purity of the target product was of 99.5%,the overall yield was of 76.3%.The structure of(S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline was confirmed by melting point,MS and^1H NMR.This process has many advantages including simple in operation,without special equipment requirements,and suitable for industrial production.

关 键 词：琥珀酸索利那新 (S)-1-苯基-1 2 3 4-四氢异喹啉 工艺改进 

分 类 号：TQ253.23[化学工程—有机化工]