METHOD FOR PREPARING ZIDOVUDINE AND INTERMEDIATE THEREOF

摘要

The present invention relates to a method for preparing zidovudine (B). The method comprises the following steps: 1) 2'-halothymidine (A) is used as the raw material to obtain a compound of formula (I) by protecting the hydroxyl group thereof in the 5'-position; 2) the compound of formula (I) is dehalogenated to obtain a compound of formula (II); 3) the compound of formula (II) is protected by the acylation of the hydroxyl group in the 3'-position to obtain a compound of formula (III); 4) the compound of formula (III) is subjected to an elimination reaction to obtain a compound of formula (IV); 5) the compound of formula (IV) is subjected to an azidation reaction to obtain a compound of formula (V); and 6) the compound of formula (V) is deprotected to obtain zidovudine (B); the reaction formula of the abovementioned routes being shown in (C). In the formulae: X is a halogen, P₁ is a protecting group for hydroxyl; and P₂ is C₁-C₄ alkylsulfonyl, fluoro-C₁-C₄ alkylsulfonyl, arylsulfonyl or -CS-R, wherein R is C₁-C₄ alkyl. The present invention also relates to the intermediate of general formula (I), wherein X and P₁ are defined as stated above.