摘要 |
<p>PURPOSE:To obtain N'-(2-tetrahydrofuryl)-5-fluorouracil usable as an anticarcinogen, by ring closure of a trimethylsilyl compound of a novel unacil derivative in the presence of a Lewis acid, e.g. SnCl4, etc. CONSTITUTION:A novel compound of formulas Ia and Ib, obtained by reacting a novel compound of formula I: (R is alkyl group) with a silylating agent at room temperature or under heating, is subjected to ring closure in the presence of a Lewis acid, e.g. BF3, SnCl4, etc. in a suitable solvent, preferably at -40 to 30 deg.C to form a compound of formula II. The compound of formula I can be obtained by reaction 2,4-bistrimethyl-silyl-5-fluorouracil with 4-trimethyl-silyloxybutyraldehyde dimethylacetal in the prsence of SnCl4.</p> |