| 摘要 |
PURPOSE:To shorten the reaction time, and to improve the purity of the product in the preparation of an aminoalkylthiol useful as a raw material of pharmaceuticals by the hydrolysis of 2-mercaptothiazoline compound, by terminating the reaction at a specific range of conversion. CONSTITUTION:The objective compound of formula II (R<1>, R<2>, R<3> and R<4> are H, lower alkyl or hydroxy-substituted lower alkyl) is prepared in high purity, by hydrolyzing a 2-mercaptothiazoline compound of formulaIwith a hydrohalogenic acid (HX), terminating the reaction when the conversion reaches 80-95%, and recrystallizing the resultant crude aminoalkylthiol with an organic solvent. The hydrohalogenic acid is e.g. hydrofluoric acid, hydrochloric acid, etc., and its amount is 4-8mol per 1mol of the 2-mercaptothiazoline compound. EFFECT:The hydrolytic conversion of as high as 80-95% can be attained easily by suppressing the successive reaction through intermediates and carrying out the direct reaction preferentially. |
