| 摘要 |
<p>NEW MATERIAL:5-Fluorouracil derivatives of formulaI[either R1 or R2 is formula II (R<3> is H, alkyl, cycloalkyl, aryl) and the other is H]. EXAMPLE: 1-(5-Fluoro-1H-2-oxopyrimidiene-4-yl-beta-D-galactopyranouronic acid. USE:Low-toxicity carcinostatic agents. PREPARATION:The condensation between 5-fluorouracil metal salt of formula III (R<5> is hydroxyl group-protecting group that can be eliminated by reduction; M is metal) and a halogenogalactopyranouronic ester derivative of formula IV (R<4> is alkyl, aryl; R<6> is hydroxyl-protecting group) gives the compound of formula V, from which protecting groups are removed to afford the compound of formulaI.</p> |
