| 摘要 |
PROBLEM TO BE SOLVED: To obtain the novel subject compound that comprises racemicβD,L-2- hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane or its resolved enantiomers and has antiviral activity. SOLUTION: This compound is (±)-β-D,L-2-hydroxymethyl-5-(5-fluorocytosin-1- yl)-1,3-oxathiolane represented by formula I [R1 and R2 are each H, an alkyl, a carboxylic ester, a (substituted) phenyl, sulfonate ester, amino acid ester; either R1 or R2 is H] and its resolved enantiomers and is useful as an antiviral agent effective for treatment of human HIV and HBV infections. This compound is prepared by ozonolysis of an allyl ether, reaction of the product with mercaptoacetic acid, followed by reduction of the product and the reaction of 1,3-oxathiolane (reduction product) with 5-fluorocytosin). |
