Regioselective protection of 10-deacetylbaccatin III and semi-synthesis of paclitaxel

被引:6
作者
Hu, Zhang [1 ,2 ]
Ou, Li Li [1 ]
Zhang, Guo Lin [1 ]
Yu, Yong Ping [1 ]
机构
[1] Zhejiang Univ, Coll Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China
[2] Guangdong Ocean Univ, Coll Sci, Zhanjiang 524088, Peoples R China
关键词
paclitaxel; protecting group; 1,1'-thiocarbonyldiimidazole; regioselective; semi-synthesis;
D O I
10.1016/j.cclet.2007.11.016
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Semi-synthesis of paclitaxel was achieved in four steps from 10-deacetylbaccatin In (10-DAB III). The key steps are the regioselective protection at the hydroxyl group at C-7 of 1 O-DAB III, using 1, 1'-thiocarbonyldiiniidazole as a selective reagent, and the deprotection of the protected paclitaxel with a mixture of p-toluenesulfonic acid and 0.1 mol/L aqueous hydrochloride. (c) 2007 Yong Ping Yu. Published by Elsevier B. V. on behalf of Chinese Chemical Society. All rights reserved.
引用
收藏
页码:130 / 132
页数:3
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