发明名称 Process for the Preparation of Voriconazole and Analogues Thereof
摘要 The present invention provides a process for preparing a compound of formula: (Formula XI and XII) (XI) (XII) wherein X, Y, Z, A, B and E are as defined herein, by reacting a compound of formula: (Formula XIII) (XIII) with a compound of formula: (Formula XIV and XV) (XIV) (XV) respectively, in the presence of a transition metal catalyst, a ligand suitable for use with 15 the catalyst and a reducing agent. The invention also provides novel intermediates.;
申请公布号 US2015239867(A1) 申请公布日期 2015.08.27
申请号 US201314431319 申请日期 2013.10.08
申请人 PFIZER IRELAND PHARMACEUTICALS 发明人 Burrell Adam James Musgrave;O'Neill Padraig Mary;Pettman Alan John
分类号 C07D403/06;C07D239/30 主分类号 C07D403/06
代理机构 代理人
主权项 1. A process for preparing a compound of formula: wherein: X is H, halo, —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), —Si(R3)3 [wherein R3 is, independently in each case, C1-C6 alkyl, Aryl or Aryl(C1-C6 alkyl)], —O(C1-C6 alkyl), —OAryl, —S(C1-C6 alkyl), —OSO2(C1-C6 alkyl), —NNSO2(C1-C6 alkyl) or —SAryl; Y is H, halo, —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), —Si(R3)3 [wherein R3 is as defined above], —O(C1-C6 alkyl), —OAryl, —S(C1-C6 alkyl), —OSO2(C1-C6 alkyl), —NHSO2(C1-C6 alkyl) or —SAryl; Z is optionally substituted heteroaryl, —Si(R3)3 (wherein R3 is as defined above), —OH, a protected hydroxyl group, halo, nitro, cyano, —SH, a protected thio group, C1-C6 alkyl or C1-C6 alkoxy; A is O, S or NH; B is phenyl substituted by one or more halo atoms; and D is a halo atom; by reacting a compound of formula: wherein Z and B are as defined above, with a compound of formula: respectively, wherein X, Y, A and D are as defined above, in the presence of a transition metal catalyst, a ligand suitable for use with the catalyst and a reducing agent.
地址 County Cork IE