PROCESS FOR PREPARING TORISEL

摘要

A process for preparing Torisel, which is a derivative of Rapamycin, is provided. The process comprises the following steps: acetalating 2,2-dihydroxymethylpropionic acid with substituted or unsubstituted aromatic aldehyde in the presence of p-toluenesulfonic acid as catalyst to form the intermediate II; reacting the obtained intermediate with 2,4,6-trichlorobenzoyl chloride; then esterifying the obtained chloride with Rapamycin and finally deprotecting the diol to provide the product Torisel with yield over 35.6%. The aromatic aldehyde is one selected from benzaldehyde, p-methoxybenzaldehyde, p-chlorobenzaldehyde and p-trifluoromethyl benzaldehyde.