含β-D-糖苷的5-氟尿嘧啶类抗肿瘤药物的合成

Synthesis of β-D-glucoside-containing 5-fluorouracil derivatives

以糖为原料,经过乙酰化、溴化得到溴代糖.以所得的溴代糖与5-氟尿嘧啶-1-基-乙酸及N1-(2-呋喃烷基)-5-氟尿嘧啶通过酯化、N-烷基化反应,合成了8个新型含糖苷的5-氟尿嘧啶类衍生物,采用IR、MS和1HNMR表征了目标化合物的结构.

Eight novel glucoside-containing 5-fluorouracil derivatives were synthesized by the reaction of bromoacetylcarbohydrate with (5-fluoro-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-acetic acid or 5-fluoro-1-(tetrahydro-furan-2-yl)-1H-pyridine-2,4-dione. Their structures were confirmed by IR, MS and ~1H NMR.