工业高纯度兰索拉唑的合成工艺改进

Improved Synthesis of Industrial High-purity Lansoprazole

目的：改进兰索拉唑的合成工艺．方法：以2-氯甲基-3-甲基-4-（三氟乙氧基）吡啶盐酸盐与2-巯基苯并咪唑缩合，高收率（97％）地获得高纯度硫醚化合物；以间氯过氧苯甲酸为氧化剂制得兰索拉唑，收率达81％．结果：目标化合物结构经^1H—NMR和MS确证．设计的合成路线及工艺操作简单，适合工业化生产．

2-Chloromethyl-3-methyl-4-（ 2,2,2-trifluoroethoxy ） pyridine hydrochloride and 2- mercaptobenzimidazole were condensed with sodium hydroxide as a condensation agent in a high yield of 97% to afford a thioether compound, which was oxidize catalytically with metachloroperbenzoic acid to prepare Lansoprazole in a yield of 81%. Their structures were confirmed by 1HNMR and MS. This improved process reduced the reaction steps, and was suitable for industrial manufacturing.