IMPROVEMENT IN THE PRODUCTION OF IMIDAZOLE DERIVATIVES AND NOVEL INTERMEDIATES OF THE DERIVATIVES
    8.
    发明公开
    IMPROVEMENT IN THE PRODUCTION OF IMIDAZOLE DERIVATIVES AND NOVEL INTERMEDIATES OF THE DERIVATIVES 审中-公开
    咪唑提高了生产及其衍生物的新的中间体

    公开(公告)号:EP1477487A1

    公开(公告)日:2004-11-17

    申请号:EP03705258.6

    申请日:2003-02-18

    申请人: Azwell Inc.

    IPC分类号: C07D401/06 C07F9/6506

    摘要: The invention provides an improvement in the production of imidazole derivatives including histamine H 3 agonist immepip and histamine H 3 antagonist VUF4929. Desired imidazole derivatives can be easily obtained in high yield by using novel intermediates represented by the general formula (I):
    wherein R 1 is an amino-protecting group; R 2 and R 3 are each independently hydrogen, lower alkyl, or hydroxy-(lower alkyl); R 4 is lower alkyl, halogenated lower alkyl, or substituted or unsubstituted phenyl; and A is C 1-3 alkylene.

    摘要翻译: 本发明提供了在生产包含组胺H3激动剂immepip和组胺H3拮抗剂VUF4929咪唑衍生物的改进。 期望的咪唑衍生物可以以高产率通过使用由通式(I)表示的新的中间体很容易地获得: worin - [R <1>是氨基保护基; [R <2>和R <3>各自unabhängig氢,低级烷基,或羟基(低级烷基); [R <4>是低级烷基,卤代低级烷基,或substituiertem奥德unsubstituiertem苯基; 且A是C 1-3亚烷基。

    ELECTRONICALLY TUNED LIGANDS
    9.
    发明授权
    ELECTRONICALLY TUNED LIGANDS 有权
    电子相合的配体

    公开(公告)号:EP1218388B1

    公开(公告)日:2004-01-28

    申请号:EP00959804.6

    申请日:2000-09-05

    发明人: BUSACCA, Carl

    摘要: A phosphino- or arsenoamidine of Formula (1) M is Phosphorus or Arsenic (P, As); X, Y, and Z can be independently selected from hydrogen, alkyl, aryl (pendant or fused), halogen, alkoxy (C1-C10), cyano, nitro, amino, alkylamino, dialkylamino, -CO2H, -CO(lower alkoxy), -CO(lower alkyl), -NCOH, -NCO(lower alkyl), NSO2(alkyl), - NSO2(aryl), hydroxy, alkyl, sulfonoxyalkyl, sulfonoxyaryl, or alkoxyalkyl; R1 is hydrogen, C1-C10 alkyl, branched alkyl or cycloalkyl; aryl, substituted aryl, heteroaryl or substituted heteroaryl where the heteroatoms may include atoms of nitrogen, oxygen, or sulfur, may be acyl, aroyl, substituted aroyl, heteroaroyl, or substituted heteroaroyl, or SO2R4 where R4 is chosen from the group alkyl, aryl, heteroaryl, substituted aryl or substituted heteroaryl groups in direct attachment, with the provisos that R2 and R3 can be the same or different and are hydrogen, aryl or heteroaryl as defined above, substituted aryl or heteroaryl as defined (with substituents as defined below), alkyl, branched alkyl, cycloalkyl, benzyl, subtituted benzyl, with substituents as defined for aryl, or R2 and R3 together may form a fused carbocyclic ring, Ring B is an imidazoline ring or a tetrahydropyrimidine ring.