左旋泮托拉唑钠的合成工艺研究  

Synthesis of(S)-(-)-Pantoprazole Sodium

作　　者：金龙[1,2] 胡鸿雨[1] 郑人卫[1] 严晓阳[1] 阳学文 熊国强 郑绍成[1] 

机构地区：[1]浙江师范大学行知学院,浙江金华321004 [2]浙江普洛得邦制药有限公司,浙江东阳322118

出　　处：《精细化工中间体》2017年第2期52-54,共3页Fine Chemical Intermediates

摘　　要：以2-氯甲基-3,4-二甲氧基吡啶盐酸盐与5-二氟甲氧基-2-巯基-1H-苯并咪唑为起始原料在氢氧化钠水溶液条件下缩合得到中间体5-二氟甲氧基-2-[[(3,4-二甲氧基-2-吡啶基)甲基]硫基]-1H-苯并咪唑,经过Sharpless不对称氧化得到粗品左旋泮托拉唑钠,再用丙酮重结晶,即可制得高纯度左旋泮托拉唑钠,总收率约65.5%,纯度99.90%。5-Difluoromethoxy-2-[[（3,4-dimethoxy-2-pyridyl）methyl]thio] -1H-benzimidazole was prepared using dimethoxypyridine hydrochloride and 5-difluoromethoxy-2-mercapto-1H-benzimidazole as the starting materials in aqueous sodium hydroxide. This obtained intermediate was then subjected to Sharpless asymmetric oxidation to give crude Pantoprazole sodium, and the. high purity levopantoprazole sodium then was obtained by recrystallization using acetone as the solvent. The total yield of the final product was up to 65.5% with a purity of 99.9%.

关 键 词：巯基物 缩合 左旋泮托拉唑钠 Sharpless不对称氧化 

分 类 号：R914[医药卫生—药物化学]