| 摘要 |
PROBLEM TO BE SOLVED: To provide a new 1,3-oxathiolane nucleoside analog effective for the treatment of viral infection diseases, especially for inhibiting the replication of retroviruses such as human immunodeficiency virus (HIV'S). SOLUTION: The objective compound is the antipode of the compound of formula I, concretely (-)-(2R,cis)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5- yl)-(1H)-pyrimidin-2-one or its pharmacologically permissible derivative. The compound has considerably low cytotoxicity compared with other antipode. The compound of the formula I can be produced e.g. by the base exchanging reaction of a compound of the formula II (B is a base convertible to cytosine). The (-)-antipode of the formula I can be produced in a state essentially free from the corresponding (+)-antipode, i.e., the content of the (+)-antipode is about <5%w/w, preferably <2%w/w and especially preferably <1%w/w. |
