Process For the Preparation of Enantiomerically Pure1-Substitued-3-Aminoalcohols

摘要

A process for the preparation of enantiomerically pure 1-substituted-3-amino-alcohols, particularly of (S)-(-)- and (R)-(+)-3-N-methylamino-1-(2-thienyl)-1-propanol, by asymmetrically hydrogenating salts of a carboxylic acids with an aminoketone of the formula: wherein R¹ is 2-thienyl, 2-furanyl or phenyl, each optionally substituted with one or more halogen atoms and/or one or more C_1-4-alkyl or C_1-4-alkoxy groups, and wherein R² is C_1-4-alkyl or phenyl, each optionally substituted with one or more halogen atoms and/or one or more C_1-4-alkyl or C_1-4-alkoxy groups. The corresponding aminoalcohols are obtained by subsequent hydrolysis of their salts. Salts of a carboxylic acid with the aminoketones and the aminoalcohols obtained by asymmetrically hydrogenating the aminoketones, respectively.