具有酰基或氨基甲酰基结构的5-氟尿嘧啶衍生物的合成及抗肿瘤活性

Synthesis and Antitumor Activity of 5-Fluorouracil Derivatives with Acyl or Carbamoyl Structure

5-氟尿嘧啶(5-FU)首先由 Duschinsky 和Pleven 合成。作为一种广谱性的抗肿瘤临床药物,其主要缺点是脂溶性小。

Six new 5-fluorouracil derivatives with acyl or carbamoyl structure were synthesized and structurally confirmed by 1~H NMR,IR,UV spectra data and elemental analyses.It was shown that reaction temperature,reactant ratio and the property of acylating agentshave significantly influence on the acylation of 2,4-bis(trimethylsilyl)-5-fluorouracil withacylating agents.Antitumor activity of the new prepared 5-fluorouracil derivatives havealso been given.