首页> 外国专利> PROCESS FOR PREPARATION OF SALTS OF S-ENATIOMER OF 5-METHOXY-2-(4-METHOXY-3,5-DIMETHYL-2-PYRIDINYLMETHYL)SULFINYL -1H-BENZIMIDAZOLE SUBSTANTIALLY FREE OF SULFONE IMPURITY

PROCESS FOR PREPARATION OF SALTS OF S-ENATIOMER OF 5-METHOXY-2-(4-METHOXY-3,5-DIMETHYL-2-PYRIDINYLMETHYL)SULFINYL -1H-BENZIMIDAZOLE SUBSTANTIALLY FREE OF SULFONE IMPURITY

机译:基本上不含砜杂质的5-甲氧基-2-[(4-甲氧基-3,5-二甲基-2-吡啶基甲基)亚磺酰基-1H-苯并咪唑的S-对映体的盐的制备方法

摘要

The present provides alkali and alkaline earth metal salts of S-enantiomer of 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinylmethyl)sulfinyl]-1H-benzimidazole, substantially free of sulfone impurity, and a process for prparation thereof comprising a) enantioselective oxidation of the prochiral sulfide, 5-methoxy-2-(4-methoxy-3,5-dimethyl-2-pyridinylmethylthio-1H-bezimidazole to form S-enantiomer of 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinylmethyl)sulfinyl]-1H-benzimidazole; b) reacting the S-enantiomer formed in step 'a' with salts alkali or alkaline earth metals to form the salt of S-enantiomer of 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinylmethyl)sulfinyl]-1H-benzimidazole; c) removing the sulfone impurity from the alkali or alkaline earth metal salt formed in step 'b' by treatment with a solvent system, said solvent system comprising an organic solvent selected from ketone and nitrile, d) and isolating the alkali or alkaline earth metal salt of S-enantiomer of 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinylmethyl)sulfinyl]-1H-benzimidazole; which is substantially free of sulfone impurity, by conventional means. The solvent system of the process of the present invention can further comprise an aqueous salt solution of a neutral salt of alkali or alkaline earth metal.
机译:本发明提供了基本上不含砜杂质的5-甲氧基-2-[(4-甲氧基-3,5-二甲基-2-吡啶基甲基)亚磺酰基] -1H-苯并咪唑的S-对映体的碱金属和碱土金属盐,和其制备方法,包括:a)手性硫化物5-甲氧基-2-(4-甲氧基-3,5-二甲基-2-吡啶基甲硫基-1H-苯并咪唑)的对映选择性氧化,以形成5-甲氧基-2的S-对映体-[[(4-甲氧基-3,5-二甲基-2-吡啶基甲基)亚磺酰基] -1H-苯并咪唑; b)使步骤'a'中形成的S对映异构体与碱金属或碱土金属盐反应形成S盐-5-甲氧基-2-[((4-甲氧基-3,5-二甲基-2-吡啶基甲基)亚磺酰基] -1H-苯并咪唑的对映异构体; c)通过用溶剂系统处理从步骤“ b”中形成的碱金属或碱土金属盐中除去砜杂质,所述溶剂系统包含选自酮和腈的有机溶剂,d)并分离碱金属或碱土金属5-甲氧基-2-[(4-甲氧基-3,5-二甲基-2-吡啶基甲基)亚磺酰基] -1H-苯并咪唑的S-对映体的盐;通过常规方法基本上不含砜杂质。本发明方法的溶剂体系可以进一步包含碱金属或碱土金属的中性盐的盐水溶液。

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