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-氟为原料经硅醚化、和四乙酰核糖缩合、皂化、酮缩醇形成、碘化、氢解及水解等反应合成了去氧氟苷。本法工艺简便、条件缓和、原料易得、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料，经成盐、环合反应得到5-氮杂，5-氮杂经硅烷化保护后，与乙酰化的核糖成苷，再脱保护基得到氮杂苷。