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| Regioselective protection of 10-deacetylbaccatin Ⅲ and semi-synthesis of paclitaxel | |
| 引用本文： | Zhang Hu Li Li Ou Guo Lin Zhang Yong Ping Yu. Regioselective protection of 10-deacetylbaccatin Ⅲ and semi-synthesis of paclitaxel[J]. 中国化学快报, 2008, 19(2): 130-132. DOI: 10.1016/j.cclet.2007.11.016 |
| 作者姓名： | Zhang Hu Li Li Ou Guo Lin Zhang Yong Ping Yu |
| 作者单位： | a College of Pharmaceutical Science, Zhejiang University, Hangzhou 310058, China;b College of Science, Guangdong Ocean University, Zhanjiang 524088, China |
| 基金项目： | Acknowledgments Yong Ping Yu thanks the Foundation of NNSFC（No. 20572098）, NSFZJ（No. Z405037） and NCET-05-0523 |
| 摘 要： | Semi-synthesis of paclitaxel was achieved in four steps from 10-deacetylbaccatin HI （10-DAB HI）. The key steps are the regioselective protection at the hydroxyl group at C-7 of 10-DAB HI, using 1,1′-thiocarbonyldiimidazole 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. |
| 关 键 词： | 保护作用 半合成 盐酸 化学工业 |
| 收稿时间： | 2007-08-26 |
Regioselective protection of 10-deacetylbaccatin III and semi-synthesis of paclitaxel |
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| Zhang Hu, Li Li Ou, Guo Lin Zhang,Yong Ping Yu,. Regioselective protection of 10-deacetylbaccatin III and semi-synthesis of paclitaxel[J]. Chinese Chemical Letters, 2008, 19(2): 130-132. DOI: 10.1016/j.cclet.2007.11.016 | |
| Authors: | Zhang Hu Li Li Ou Guo Lin Zhang Yong Ping Yu |
| Affiliation: | a College of Pharmaceutical Science, Zhejiang University, Hangzhou 310058, China;b College of Science, Guangdong Ocean University, Zhanjiang 524088, China |
| Abstract: | Semi-synthesis of paclitaxel was achieved in four steps from 10-deacetylbaccatin III (10-DAB III). The key steps are the regioselective protection at the hydroxyl group at C-7 of 10-DAB III, using 1,10-thiocarbonyldiimidazole 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. # 2007 Yong Ping Yu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved. |
| Keywords: | Paclitaxel Protecting group 1 10-Thiocarbonyldiimidazole Regioselective Semi-synthesis |
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