摘要
以10脱乙酰巴卡亭Ⅲ为起始原料,将其转化成7三乙基硅烷10脱乙酰巴卡亭Ⅲ,然后乙酰化成7三乙基硅烷巴卡亭Ⅲ,用市售的紫杉醇侧链N苯甲酰(2R,3S)3苯基异丝氨酸在DCC和DAMP作用下与其偶联。
The starting material was 10 deacetylbaccatin Ⅲ,and this was converted to 7 triethylsilyl 10 deacetylbaccatin Ⅲ and then acetylated to give 7 triethylsilyl baccatin Ⅲ,which was then coupled with the commercially available side chain N benzoyl (2 R,3S ) phenylisoserine in the presence of DCC and DMAP.Removal of the protecting group with 0 5% HCl gave Taxol in high yield.
出处
《中国药物化学杂志》
CAS
CSCD
1999年第1期56-58,共3页
Chinese Journal of Medicinal Chemistry
关键词
紫杉醇
脱乙酰巴卡亭Ⅲ
半合成
Taxol
10 deacetylbaccatin Ⅲ
N benzoyl (2 R,3S ) phenylisoserine
semisynthesis