Patent ID: 8722880
Filing Date: 2014-05-13
Classification: C07F

Abstract:
1. A method for preparing 42-(dimethylphosphinate) Rapamycin (Ridaforolimus) of the following formula I, comprising the following steps: (a) reacting Rapamycin of the following formula II with a silane compound in a first basic condition to obtain a compound of the following formula IV: (b) deprotecting the compound of the formula IV in a first acid condition to obtain a compound of the following formula V: (c) reacting the compound of the formula V with Dimethylphosphinic chloride in a second basic condition to perform a phosphorylation reaction to obtain a compound of the following formula VI: (d) hydrolyzing the compound of the formula VI in a second acid condition to obtain Ridaforolimus of the formula I, wherein each R