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

Zhang Hu Li Li Oua Guo Lin Zhang Yong Ping Yu

引用本文: Zhang Hu,  Li Li Oua,  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 shu
Citation:  Zhang Hu,  Li Li Oua,  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 shu

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

  • 基金项目:

    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 Ⅲ (10-DAB Ⅲ).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.

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  • 收稿日期:  2007-08-26
通讯作者: 陈斌, bchen63@163.com
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    沈阳化工大学材料科学与工程学院 沈阳 110142

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