Liang Chengyuan, Ju Weihui, Ding Shunjun, Sun Han, Mao Gennian
Faculty of Pharmacy, Shaanxi University of Science & Technology, 6 Xuefu Road, Xi'an 710021, China.
Molecules. 2017 Jan 5;22(1):84. doi: 10.3390/molecules22010084.
An effective synthesis of nucleosides using glycosyl chlorides as glycosyl donors in the absence of Lewis acid has been developed. Glycosyl chlorides have been shown to be pivotal intermediates in the classical silyl-Hilbert-Johnson reaction. A possible mechanism that differs from the currently accepted mechanism advanced by Vorbrueggen has been proposed and verified by experiments. In practice, this catalyst-free method provides easy access to Capecitabine in high yield.
已开发出一种在无路易斯酸的情况下使用糖基氯作为糖基供体有效合成核苷的方法。糖基氯已被证明是经典硅基-希尔伯特-约翰逊反应中的关键中间体。已提出一种不同于目前由沃布吕根提出的被广泛接受的机理，并通过实验进行了验证。实际上，这种无催化剂方法能够以高收率轻松制得卡培他滨。
