An efficient method for the introduction of a methyl group in the 5-position of uridine derivatives is described. This method involves three steps: protection of 5-halogenouridines 4 and 5 with hexamethyldisilazane, a palladium-catalyzed cross-coupling of the pertrimethylsilylated nucleosides with trimethylaluminum, and subsequent deprotection to afford the corresponding thymidine derivatives 6 in high overall yields.
描述了一种在
尿苷衍
生物的5-位引入甲基的有效方法。该方法包括三个步骤:用
六甲基二硅氮烷保护5-卤代
尿苷4和5,接着通过
钯催化的交叉偶联反应与全三甲基
硅基化的核苷酸与
三甲基铝反应,最后进行去保护,以高总收率得到相应的
胸苷衍
生物6。