PREPARATION METHOD OF 4-AMINO-1-HYDROXYBUTYLIDENE-1,1-BISPHONIC ACID AND SALTS THEREFROM

摘要

PURPOSE: A preparation method of 4-Amino-1-hydroxybutylidene-1,1-bisphonic acid and/or salts thereof is provided to give a prominent effect for osteoporosis and to enable it economically and safely. CONSTITUTION: 4-Amino-1-hydroxybutylidene-1,1-bisphonic acid comprises reaction of γ -amino butyric acid with water and phosphorus chloride mixture; and withdrawal of 4-Amino-1-hydroxybutylidene-1,1-bisphonic acid or salts thereof. During the reaction, a phosphorus intermediate is generated and methane sulfonic acid is used for a solvent to dissolve the phosphorus intermediate. The reaction is performed in air. And 4-Amino-1-hydroxybutylidene-1,1-bisphonic acid or the salts manufacturing method thereof comprises an addition step of sodium hydroxide of 0.9-1.0 times of 4-Amino-1-hydroxybutylidene-1,1-bisphonic acid molecular weight; and a gradually cooling step of the reactants after elevating the temperature up to a predetermined point.