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ChemicalBook CAS DataBase List Cabazitaxel

Cabazitaxel synthesis

5synthesis methods
Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity. Cabazitaxel binds to and stabilizes tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, this agent is a poor substrate for the membrane-associated, multidrug resistance (MDR), P-glycoprotein (P-gp) efflux pump and may be useful for treating multidrug-resistant tumors. In addition, cabazitaxel penetrates the blood-brain barrier (BBB).
Synthetic Routes
  • ROUTE 1
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    Jing, Yun-rong; Zhou, Wei; Li, Wan-liang; Zhao, Lin-xiang; Wang, Yong-feng; Bioorganic & Medicinal Chemistry, Volume 22, Issue 1, Pages 194-203, Journal, 2014

  • ROUTE 2
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    Zhang, Guoning; Fang, Weishuo Journal of Chinese Pharmaceutical Sciences Volume 21 Issue 5 Pages 472-476 Journal 2012

  • ROUTE 3
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    Li, Caihong; Qiu, Yatao; Li, Xing; Liu, Nianjin; Yao, Zhiyi Bioorganic & Medicinal Chemistry Letters Volume 24 Issue 3 Pages 855-859 Journal; 2014

  • ROUTE 4
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    Method for preparation of Cabazitaxel Sun, Xiaoqiang; Chen, Xin; Yang, Haitao; Miao, Chunbao Assignee Changzhou University, Peop. Rep. China 2011 Patent Information Dec 21, 2011 CN 102285947 A

  • ROUTE 5
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    Simo, Ondrej; Vraspir, Pavel; Holas, Tomas; Jegorov, Alexandr; Gabriel, Roman. Processes for preparation of solid state forms of cabazitaxel. Assignee Plus Chemicals SA, Switz.; Teva Pharmaceuticals USA, Inc. WO 2012142117. (2012).

  • ROUTE 6
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    Liu, Ping; Yuan, Jiandong. Method for synthesis of Cabazitaxel from 10-deacetylbaccatin III. Assignee Xintai Pharmaceutical (Suzhou) Co., Ltd., Peop. Rep. China. CN 102659721. (2012).

  • ROUTE 7
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    Sethi, Madhuresh Kumar; Mahajan, Sanjay; Mara, Bhairaiah; Veera, Upendranath. Process for the preparation of cabazitaxel and its solvates. Assignee Mylan Laboratories Ltd., India. IN 2013CH05688. (2016).

  • ROUTE 8
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    Hsiao, Tsungyu; Henschke, Julian Paul; Tseng, Hsinchang. Process for the preparation of cabazitaxel, and 1,3-dithiolane or 1,3-dithiane intermediates thereof. Assignee ScinoPharm Taiwan Ltd., Taiwan. US 20130116444. (2013).

202112075770168252.jpg

Jing, Yun-rong; Zhou, Wei; Li, Wan-liang; Zhao, Lin-xiang; Wang, Yong-feng; Bioorganic & Medicinal Chemistry, Volume 22, Issue 1, Pages 194-203, Journal, 2014

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