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(2S,3R)-1-二甲氨基-3-(3-甲氧基苯基)-2-甲基戊-3-醇的合成工艺研究
引用本文:谢 应,黄淑云,李兴伟,方 玲.(2S,3R)-1-二甲氨基-3-(3-甲氧基苯基)-2-甲基戊-3-醇的合成工艺研究[J].现代药物与临床,2011,26(6):461-463.
作者姓名:谢 应  黄淑云  李兴伟  方 玲
作者单位:谢应 (天津中医药大学,天津,300193) ; 黄淑云 (天津药物研究院化学制药研究部,天津,300193) ; 李兴伟 (天津药物研究院化学制药研究部,天津,300193) ; 方玲 (天津中医药大学,天津,300193) ;
摘    要:目的 对(2S,3R)- 1-二甲氨基-3-(3-甲氧基苯基)-2-甲基戊-3-醇合成工艺进行研究.方法 以3-戊酮为起始原料,经Mannich反应、手性拆分、Grignard反应等步骤合成(2S,3R)-1-二甲氨基-3-(3-甲氧基苯基)-2-甲基戊-3-醇,并对化学拆分进行工艺优化.结果 合成(2S,3R)-1...

关 键 词:(2S  3R)-  1二甲氨基-3  -(3-甲氧基苯基)-2-甲基戊-3-醇  化学合成  Grignard反应  Mannich反应  手性拆分

Synthesis of (2S,3R)-1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol
XIE Ying,HUANG Shu-yun,LI Xing-wei and FANG Ling.Synthesis of (2S,3R)-1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol[J].Drugs & Clinic,2011,26(6):461-463.
Authors:XIE Ying  HUANG Shu-yun  LI Xing-wei and FANG Ling
Institution:1.Tianjin University of Traditional Chinese Medicine,Tianjin 300193,China 2.Centre for Chemical Pharmaceutical Research,Tianjin Institute of Pharmaceutical Research,Tianjin 300193,China
Abstract:Objective To study the synthetic technology of (2S,3R)-1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol. Methods 3-Pentanone was taken as the starting material, (2S,3R)-1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol was obtained after a series of chemical reactions including Mannich reaction, resolution, Grignard reaction, and so on. At the same time, the procedure of chiral resolution was optimized. Results (2S,3R)-1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol was synthesized with an overall yield of 30.6%. Conclusion The improved procedure can increase the yield of product and reduce the waste of raw material.
Keywords:(2S  3R)-1-dimethylamino-3-(3-methoxyphenyl)-2methylpentan-3-ol  chemical synthesis  Grignard reaction  Mannich reaction  chiral resolution
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