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
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
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
Regioselective protection of 10-deacetylbaccatin Ⅲ and semi-synthesis of paclitaxel
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.
English
Regioselective protection of 10-deacetylbaccatin Ⅲ and semi-synthesis of paclitaxel
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 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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Key words:
- Paclitaxel
- / Protecting group
- / 1,1'-Thiocarbonyldiimidazole
- / Regioselective
- / Semi-synthesis
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