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Methods and useful intermediates for paclitaxel synthesis from c-7, c-10di-cbz 10-deacetylbaccatin iii

CA 2331094 A1 · Owner: Mcchesney, James D. · Inventors: Sisti, Nicholas J.; Mcchesney, James D.; Zygmunt, Jan

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Abstract From the Canadian patent

The present invention relates to a method of producing paclitaxel or a paclitaxel analog comprising the esterification of C-7 C-10 di-CBZ baccatin , III with an N-carbamate protected C-2-protected 3-phenyl isoserine side chain. The C-7, C-10 carbobenzyloxy groups are then replaced with hydrogen and an acyl group is substituted at the C-3' nitrogen. The resulting compound is acylated at the C-10 hydroxyl position and deprotected at the C-2' position , by replacing the hydroxyl protecting group with hydrogen to produce paclitaxel or a paclitaxel analog. The present invention also relates to alternative methods of acylating a 10-hydroxy paclitaxel analog. The first method comprises …

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Listed from its CIPO record in Patent Yard's archive of Canadian patents past their term. Its claims, description and drawings are in the CIPO record and on Google Patents, and the Claude kit works from them.

Why it's free to use

  • Filed April 29, 1999. No grant is recorded for it in Canada; had it been granted, its 20-year term would have ended April 29, 2019.
  • A certificate of supplementary protection adds at most two years for a drug, so even that would have ended by April 29, 2021.
  • We check Canadian rights only. A patent in its family in another country could still be in force: check its family on Google Patents.
FiledApril 29, 1999
GrantedNo grant recorded
Term endedApril 29, 2019
Patent numberCA 2331094 A1
Classification (IPC)C07D305/14

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2000200220042006200820102012201420162018Application filedApril 29, 1999Term endedApril 29, 2019

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Everything on this page comes from the CIPO record linked above. Contains information licensed under the Open Government Licence – Canada.