C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 417/06 (2006.01) C07D 277/30 (2006.01) C07D 491/044 (2006.01)
Patent
CA 2404212
The present invention relates to a process for the preparation of epothilone analogs by initially forming novel ring-opened epothilones and carrying out a macrolactamization reaction thereon. The subject process is amenable to being carried out in a single reaction vessel without isolation of the intermediate compound and provides at least about a three-fold increase in yield over prior processes for preparing the desired epothilone analogs.
La présente invention concerne un procédé de préparation d'analogues d'épothilone, qui consiste dans un premier temps à former de nouveaux épothilones à noyau ouvert, puis à les soumettre à une réaction de macrolactamisation. Ce processus peut se dérouler dans une cuve à réaction unique, sans isolement d'un composé intermédiaire, et autorise des rendements de trois fois supérieurs à ceux procurés par des procédés traditionnels dans la préparation des analogues d'épothilone requis.
Guo Zhenrong
Li Wen Sen
Swaminathan Shankar
Thornton John E.
Bristol-Myers Squibb Company
Gowling Lafleur Henderson Llp
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