Process for the reduction of oxiranyl epothilones to olefinic epothilones
    5.
    发明授权
    Process for the reduction of oxiranyl epothilones to olefinic epothilones 有权
    将环氧乙酰基埃坡霉素还原为烯属埃坡霉素的方法

    公开(公告)号:US06320045B1

    公开(公告)日:2001-11-20

    申请号:US09316796

    申请日:1999-05-21

    IPC分类号: C07D49304

    CPC分类号: C07D417/06

    摘要: The invention as claimed is directed to a process for making an epothilone having the following structures from ones having an oxiranyl moiety, by reacting a compound having the latter structure with a metal or metal-assisted reagent. Said metal or metal-assisted reagent is selected from the group consisting of a) reactive metallocenes; b) [N2C(CO2Me)2, cat Rh2,(OAC)4]; c) [N2C(CO2Me)2, cat[(n-C7H15CO2)2 Rh]2]; d) [Zn—Cu, EtOH]; e) [Mg(Hg), MgBr]; f) Cr; g) [FeCl3, n-BuLi]; h) [TiCl3, LiAlH4]; i) [TiCl4, Zn]; j) [WCl6, LiAlH4,]; k) [NbCl5, NaAlH4]; l) [VCl3,Zn] and m) [WCl6, n-BuLi].

    摘要翻译: 本发明涉及通过使具有后一种结构的化合物与金属或金属辅助试剂反应制备具有下列结构的埃博霉素的方法:具有环氧乙烷基的化合物。 所述金属或金属辅助试剂选自a)反应性金属茂; b)[N2C(CO2Me)2,猫Rh2,(OAC)4]; c)[N2C(CO2Me)2,cat [(n-C7H15CO2)2 Rh] 2]; d)[Zn-Cu,EtOH]; e)[Mg(Hg),MgBr]; f)Cr; g)[FeCl 3,n-BuLi]; h)[TiCl 3,LiAlH 4]; i)[TiCl 4,Zn]; j)[WCl6,LiAlH4]; k)[NbCl 5,NaAlH 4]; l)[VCl 3,Zn]和m)[WCl 6,n-BuLi]。