| 摘要 |
<p>NEW MATERIAL:The compound of formulaI(R1 is H or 1-4C alkyl; R2 is 2- 20C bivalent aliphatic hydrocarbon group; R3 is H or alkali cation). EXAMPLE:1-[5'-(2-Aminoethylphosphoryl)-beta-D-arabinofuranosyl]cytosine. USE:An antitumor agent. It can be administered orally, and exhibits excellent activity. It is also useful as an intermediate for the synthesis of pharmaceuticals. PROCESS:The compound of formulaIis prepared by reacting the protected 1-(beta- D-arabinofuranosyl)cytosine 5'-phosphate of formula II (R4 is amino-protecting group; R5 and R6 are same or different OH-protecting group) with the amino- protected amino alcohol of formula III (R7 is amino-protecting group) to form phosphodiester bond, removing the protecting groups R4, R5, R6 and R7 from the product, and if necessary, converting the product to an alkali salt.</p> |
