Invention Grant
US07847111B2 Semi-synthetic route for the preparation of paclitaxel, docetaxel, and 10-deacetylbaccatin III from 9-dihydro-13-acetylbaccatin III
失效
用于从9-二氢-13-乙酰基浆果赤霉素III制备紫杉醇,多西他赛和10-脱乙酰基浆果赤霉素III的半合成途径
- Patent Title: Semi-synthetic route for the preparation of paclitaxel, docetaxel, and 10-deacetylbaccatin III from 9-dihydro-13-acetylbaccatin III
- Patent Title (中): 用于从9-二氢-13-乙酰基浆果赤霉素III制备紫杉醇,多西他赛和10-脱乙酰基浆果赤霉素III的半合成途径
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Application No.: US11425034Application Date: 2006-06-19
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Publication No.: US07847111B2Publication Date: 2010-12-07
- Inventor: Jian Liu
- Applicant: Jian Liu
- Applicant Address: CA Montreal, QC
- Assignee: Canada Inc.
- Current Assignee: Canada Inc.
- Current Assignee Address: CA Montreal, QC
- Agency: Benoît & Côté, s.e.n.c.
- Main IPC: C07D305/14
- IPC: C07D305/14

Abstract:
A semisynthetic route has been provided in the preparation of docetaxel and paclitaxel. This new process involves the conversion of 9-dihydro-13-acetylbaccatin III to docetaxel and paclitaxel by the step of converting 9-dihydro-13-acetylbaccatin III into 7-O-triethylsilyl-9,10-diketobaccatin III, and adding docetaxel and paclitaxel side chain precursors, respectively, to form a new class of taxane intermediates, such as 7-O-triethylsilyl-9,10-diketodocetaxel and 7-O-triethylsilyl-9,10-diketopaclitaxeltaxel. These new intermediates then by a series reduction, acetylation of the 10-hydroxyl position for paclitaxel and finally deprotection to yield docetaxel and paclitaxel, the most important anti-cancer drugs.
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