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
  • Application No.: US11425034
    Application Date: 2006-06-19
  • Publication No.: US07847111B2
    Publication 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
Semi-synthetic route for the preparation of paclitaxel, docetaxel, and 10-deacetylbaccatin III from 9-dihydro-13-acetylbaccatin III
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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