09-05-2023 дата публикации
Номер: CN116082363A
Принадлежит:
The invention discloses an alkylation synthesis method for 40-site hydroxyl of rapamycin, and belongs to the technical field of medicine synthesis. The method comprises the following steps: in an inert gas atmosphere, rapamycin, a molecular sieve and an additive are sequentially added into a microwave reaction tube, and the additive is triphenylphosphine oxide, tris (4-fluorophenyl) phosphine oxide, tris (4-methoxyphenyl) phosphine oxide, tricyclohexylphosphine oxide, triphenylphosphine sulfide, triphenylphosphine selenide or hexamethylphosphoric triamide; and then adding an alkylation reagent, alkali and an organic solvent, sealing, reacting in a microwave reaction instrument, cooling, carrying out suction filtration, washing, drying, filtering and purifying to obtain an alkylated product of 40-site hydroxyl of rapamycin. Compared with an existing alkylation modification method of rapamycin 40-site hydroxyl, the method has the advantages that the operation is simple, the cost is low, the ...
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