左旋泮托拉唑钠的合成工艺研究

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

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%.