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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%。
40-O- [2- (tert-butyldimethylsilyloxyethyl)] rapamycin was obtained by condensation reaction of rapamycin with t-butyldimethylchloroethoxysilane , Followed by deprotection of trifluoroacetic acid / dichloromethane solution system to obtain the antitumor drug everolimus, the total yield of 79%.