5-Fluorouracil Derivatives. X. : Synthesis and Antitumor Activities of α-Alkoxyalkyl-5-fluorouracils

概要

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With the aim of diminishing the toxicity of 5-fluorouracil (1) and obtaining biologically active derivatives of 1 suitable for oral administration, α-alkoxyalkyl groups were introduced at the 1-, 3-and 1,3-positions of 1. Alkoxyalkylation can be effected by four methods : (i) reaction of 1-alkoxyalkyl chloride (2) with 1,(ii) reaction of acetal with 2,4-bis (trimethylsiloxy)-5-fluoropy-rimidine, (iii) addition reaction of α-unsaturated ether with 1,(iv) aminolysis of 1-alkylthio-carbonyl-3-(1-alkoxyalkyl)-5-fluorouracil. The toxicity of the products was less than that of 1,and some of these compounds showed moderate antitumor activity against L-1210 leukemia.
社団法人日本薬学会の論文
1986-01-25