silylation

Doxifluridine was facilely synthesized from 5-fluorouracil in overall yield of 54.6% via trimethyl silylation, condensation, saponification, ketal formation, iodation, hydrogenolysis and hydrolysis.

以5-氟嘧啶为原经硅醚、和四乙酰核糖缩合、皂、酮缩醇形成、碘、及水等反应合成了去氧氟苷。本法工艺简便、条件缓和、原、成本低,总收率达54.6

Cyanoguanidine and acetylated β-D-ribose were used as starting materials to give target compound via salt formation, cyclization, silylation, coupling reaction and deprotection.

摘要以氰基胍和甲酸为原，经成盐、环合反应到5-氮杂胞嘧啶，5-氮杂胞嘧啶经硅烷保护后，与乙酰的核糖成苷，再脱保护基到氮杂胞苷。