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Intermediate for the synthesis of lansoprazole and its method of obtention.

机译:兰索拉唑合成的中间体及其获得方法。

摘要

Intermediate for the synthesis of lansoprazole and process for obtaining them. CHEMICAL FORMULA (I), called N-oxide, 2 - [[[1H-benzimidazol-2-yl] thio] methyl] -3-methyl-4- (2,2,2-trifluoroethoxy) pyridine, used as INTERMEDIATE for the synthesis of pharmaceutically active agent, antiulcer and commercial CALLING lansoprazole. METHOD FOR PREPARING (I) from the N-OXIDE 2,3-dimethyl-4-nitropyridine. PRODUCT USE PROCEDURE (I) as intermediate in the synthesis of lansoprazole wherein the N-oxide group pyridine (I) IS REDUCED BY A pyridyl phosphorus trichloride in chloroform or DIMETILFORMANIDA, GIVING 2 - [[[3- METHYL-4- (2,2,2-trifluoroethoxy) -2-pyridyl] methyl] thio] -1H-benzimidazole, and because this is oxidized to LANSOPRAZOL BY hYDROPEROXIDE tert-butyl in the presence of vanadium compound as catalyst. The invention is useful for industrially obtained lansoprazole pure and higher performance FORM.
机译:兰索拉唑合成的中间体和获得它们的方法。化学式(I),称为N-氧化物,2-[[[[1H-苯并咪唑-2-基]硫代]甲基] -3-甲基-4-(2,2,2-三氟乙氧基)吡啶,用作中间体合成药物活性剂,抗溃疡药和市售CALLING兰索拉唑。由N-氧化物2,3-二甲基-4-硝基吡啶制备(I)的方法。产品使用程序(I)作为兰索拉唑合成的中间体,其中N-氧化物基团吡啶(I)在氯仿或DIMETILFORMANIDA中被吡啶基三氯化磷还原,生成2-[[[[3- METHYL-4-(2, 2,2-三氟乙氧基)-2-吡啶基]甲基]硫基] -1H-苯并咪唑,因为在钒化合物作为催化剂存在下,过氧化氢叔丁基将其氧化为兰索拉唑。本发明可用于工业上获得的兰索拉唑纯和更高性能的FORM。

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