依维莫司的合成改进

Improved Synthesis Method of Everolimus

以雷帕霉素为原料,与叔丁基二甲基氯乙氧基硅烷进行缩合反应制得40-O-[2-(叔丁基二甲基硅氧基乙基)]雷帕霉素,再经过三氟乙酸/二氯甲烷溶液体系脱保护制得抗肿瘤药依维莫司,总收率79%。

Everolimus was synthesized from rapamycin by condensation with t-butyldimethylchloroethoxysilane to give 40-O-[2-（t-butyldimethylsilyloxyethyl）]rapamycin, followed by deprotection in the presence of trifluoroacetic acid/dichloromethane with an overall yield of about 79%.