PROCESS FOR PREPARING 4-AMINOMETHYL-3-ALKOXYIMINOPYRROLIDINE METHANE SULFONATE THROUGH REDUCED PREPARATION PROCESS

摘要

PURPOSE: A process for preparing 4-aminomethyl-3-alkoxyiminopyrrolidine methane sulfonate is provided through reduced preparation process, thereby cheaply preparing the compound without using expensive raw materials and organic solvents. CONSTITUTION: The process for preparing 4-aminomethyl-3-alkoxyiminopyrrolidine methane sulfonate represented by the formula(I) comprises the steps of: (a) reacting a compound of the formula(II) with alkoxyamine or haloalkoxyamine or salts thereof in the presence of base to prepare a compound of the formula(III); (b) reacting the compound of the formula(III) with methane sulfonate to prepare a compound of the formula(IV); and (c) adding methane sulfonate and hydrogenated catalyst into the compound of the formula(IV) to hydrogenate the compound of the formula(IV), wherein R1 is C1-C4-alkyl, or halogeno-C1-C4-alkyl; P is a protecting group such as t-butoxycarbonyl(BOC); and the base is triethylamine, tri(n-butyl)amine, diisopropylethylamine, pyridine, 4-dimethylaminopyridine, 4-(4-methyl-piperidin-1-yl)-pyridine or sodium acetate.