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(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
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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.
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)
出处 《精细化工中间体》 CAS 2020年第1期44-47,共4页 Fine Chemical Intermediates
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 solifenacin succinate (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline process improvement
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