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雷帕霉素与2-[(四氢-2H-吡喃-2-基)氧基]乙基三氟甲磺酸酯在有机碱作用下缩合得到40-O-[(四氢-2H-吡喃-2-氧基)乙基]雷帕霉素,然后直接在酸性条件下脱除缩醛保护基,最后经制备液相分离纯化得到依维莫司,总收率约66%。该路线选择性较好,反应条件温和,具有工业应用价值。
Rapamycin is condensed with 2 - [(tetrahydro-2H-pyran-2-yl) oxy] ethyl trifluoromethanesulfonate under the action of an organic base to give 40-O - [(tetrahydro- Pyran-2-yloxy) ethyl] rapamycin, and then the acetal protecting group is removed directly under acidic conditions. Finally, the obtained liquid phase is isolated and purified to obtain everolimus. The total yield is about 66%. The route selectivity is better, the reaction conditions are mild, with industrial application value.