| 摘要 |
<p>NEW MATERIAL:A compound of formulaI[R1 is formula VII or VIII (X is H, F or CH3); R2 is H or formula IX)]. EXAMPLE:1-[2-[N'-( 2-Chloroethyl )-N-nitrosoureido]-2-deoxy-beta-D-glucopyranosyl]thymine of formula X. USE:An antileukemic agent. PROCESS:An O- protected- N -protected-1-bromo-2-amino-2-deoxy-alpha- D -glucose of formula II is reacted with O-trimethylsilylated thymine, uracil or 5-fluorouracil to give a compound of formula IV, which is then subjected to the removal of the protecting groups of O atoms and N atom to afford a compound of formula V. The resultant compound of formula V is then converted into a chloroethylureide derivative to afford a compound of formula VI, which is then nitrosated by blowing N2O3 gas thereinto.</p> |
