Lipozyme TL IM催化合成Temsirolimus

Catalytic Synthesis of Temsirolimus by Lipozyme TL IM

在脂肪酶Lipozyme TL IM的催化下,2,2,5-三甲基-1,3-二氧六环-5-羧酸酐对抗生素西罗莫司的42-位羟基进行区域选择性酯化制得化合物4;4水解后合成了西罗莫司脂化物Temsirolimus,总产率83.7%。其结构经1H NMR和HR-MS确证。

Temsirolimus was prepared by regioselective esterification at the 42-hydroxy of sirolimus using 2,2,5-trimethyl-1,3-dioxane-5-carboxylic anhydride as the esterifying agent and Lipozyme TL IM as the catalyst to give intermediate 4,followed by hydrolysis.The total yield was 83.7% and the structure was confirmed by 1H NMR and HR-MS.