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    Screening Methods
    2.
    发明申请
    Screening Methods 审中-公开

    公开(公告)号：US20080039625A1

    公开(公告)日：2008-02-14

    申请号：US11718769

    申请日：2005-11-04

    申请人： Mark Lautens ,  Yuanqing Fang

    发明人： Mark Lautens ,  Yuanqing Fang

    IPC分类号： C07D209/08 ,  C07D209/10 ,  C07D401/14

    CPC分类号： C07C205/11 ,  C07C201/12 ,  C07C205/58 ,  C07C211/52 ,  C07C211/56 ,  C07D209/08 ,  C07D209/10 ,  C07D209/12 ,  C07D401/04 ,  C07D409/04 ,  C07C205/44 ,  C07C205/45 ,  C07C205/61

    摘要： Disclosed are processes for the preparation of 2-substituted indole compounds wherein the 2-substituent comprises an R4 group, wherein R4 is selected from the group consisting of monocyclic aromatic, polycyclic aromatic, monocyclic heteroaromatic, polycyclic heteroaromatic, 1° alkyl, and alkenyl, all of which are optionally substituted at one or more substitutable positions with one or more suitable substituents, and wherein R4 is bonded to the 2-position of the indole ring via a C—C bond; the process comprising reacting an orthogem-dihalovinylaniline compound of the formula (I): wherein Halo comprises Br, Cl, or I; each of the one or more R1 is independently selected from the group consisting of H, fluoro, lower alkyl, lower alkenyl, lower alkoxy, aryloxy, lower haloalkyl, lower alkenyl, —C(O)O-lower alkyl, monocyclic or polycyclic aryl or heteroaryl moiety, or R1 is an alkenyl group bonded so to as to form a 4- to 20-membered fused monocycle or polycyclic ring with the indole ring; all of which are optionally substituted with one or more suitable substituents at one or more substitutable positions; R2 comprises H, alkyl, cycloalkyl, aryl, heteroaryl, aryl-loweralkyl-, or heteroaryl-loweralkyl-, all of which are optionally substituted at one or more substitutable positions with one or more suitable substituents; R3 comprises H, alkyl, haloalkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycle, aryl-(C1-6)alkyl-, or heteroaryl-loweralkyl-, all of which are optionally substituted at one or more substitutable positions with one or more suitable substituents; with an organoboron reagent selected from the group consisting of a boronic ester of R4, a boronic acid of R4, a boronic acid anhydride of R4, a trialkylborane of R4 and a 9-BBN derivative of R4; in the presence of a base, a palladium metal pre-catalyst and a ligand under reaction conditions effective to form the 2-substituted indole compound. Also disclosed are processes for the preparation of ortho-gem-dihalovinylaniline compounds. Novel compounds prepared by the processes and novel uses of the compounds are likewise disclosed.