Kundu N G, Schmitz S A
J Pharm Sci. 1982 Aug;71(8):935-8. doi: 10.1002/jps.2600710825.
Some N-alkyl derivatives of 5-fluorouracil were designed to act as latent depot forms of 5-fluorouracil. A general and efficient method for the syntheses of the alkylated derivatives is described. As expected, the alkylated derivatives of 5-fluorouracil did not show any cytotoxicity in cell culture systems even up to 10(-4) M concentration. The synthesis of 1,3-dimethyl-5-fluoro-5,6-dihydrouracil is also described.
设计了一些5-氟尿嘧啶的N-烷基衍生物作为5-氟尿嘧啶的潜在长效剂型。描述了一种合成烷基化衍生物的通用且高效的方法。正如预期的那样,5-氟尿嘧啶的烷基化衍生物在细胞培养系统中即使浓度高达10^(-4) M也未显示出任何细胞毒性。还描述了1,3-二甲基-5-氟-5,6-二氢尿嘧啶的合成。