摘要
以β-胸苷为起始原料,5’-伯羟基采用对甲氧基苯甲酸保护,并在DEAD/PPh3体系中经过mitsuobu反应形成氧桥化合物,再与叠氮化钠发生叠氮化反应,最后脱对甲氧基苯甲酸保护基后获得目标产物齐多夫定,总收率62%。
β-Thymidine was used as the starting material. Oxygen bridge compound was formed via mitsuobu reaction from 5' -primary hydroxyl protected by p-methoxy benzoic acid in DEAD/PPh3 system. The zidovudine was obtained via azide reaction between oxygen bridge compound and sodium azide. The total yield was 62%.
出处
《应用化工》
CAS
CSCD
2011年第8期1484-1485,共2页
Applied Chemical Industry
关键词
齐多夫定
胸苷
合成
zidovudine
thymidine
synthesis