从尿核苷合成异胞苷衍生物的简便有效方法

A Simple and Efficient Method for Synthesis of Isocytidine Derivatives from Uridine

本文报道从5’-O-磺酰基2’,3’-O-异亚丙基尿核苷通过一步法合成N-烷基2’,3’-O-异亚丙基异胞苷和从5’-O-对甲苯磺酰基尿核苷合成5’-脱氧-5’-异丙氨基尿核苷.并对以上产物形成的机制作了探讨.

Isocytidine derivatives (4-8) had been synthesized in reasonable yield in one step by reaction of uridine derivatives 1, 2 and 3 with alkylamine in the presence of triethylamine at room temperature, while the reaction of 5'-O-(p-tolylsulfonyl)-uridine with isopropylamine gives 5'-deoxy-5'-isopropylaminouridine in same conditions. A plausible mechanism of the reaction is proposed.