摘要 |
Optically pure voriconazole can be prepared in a high yield by a) subjecting 1-(2,4-difluorophenyl)-2(1H-1,2,4-triazol-1-yl)ethanone to Reformatsky-type coupling reaction with a substituted thiopyrimidine derivative to obtain a desired (2R,3S)/(2S,3R)-enantiomeric pair; b) removing the thiol derivative from the enantiomer to obtain racemic voriconazole; and c) isolating the racemic voriconazole by way of optical resolution using an optically active acid. |
申请人 |
HANMI PHARM. CO., LTD.;MOON, YOUNG HO;LEE, MOON SUB;YOO, JAE HO;KIM, JI SOOK;KIM, HAN KYONG;CHOI, CHANG JU;CHANG, YOUNG KIL;LEE, GWAN SUN |
发明人 |
MOON, YOUNG HO;LEE, MOON SUB;YOO, JAE HO;KIM, JI SOOK;KIM, HAN KYONG;CHOI, CHANG JU;CHANG, YOUNG KIL;LEE, GWAN SUN |