| 摘要 |
<p>The present invention discloses a process for synthesizing Compound (I) of N<SUP>4</SUP>-acyl-5'-deoxy-5-fluorocytidine derivatives. The present invention utilizes Bis (trichloromethyl) carbobate as acylating agent for introducing protective lactone ring to the hydroxyl of saccharide moiety, and uses 5'-deoxy-5-fluorocytidine (Compound II) as starting material through key intermediate of Compound (III) and Compound (IV) to obtain target compounds through 3 steps. The process of the present invention has certain advantages such as high yield, short work-up time, available starting material, and convenience for industrial manufacture on a large scale.</p> |
