4-AMINOQUINAZOLINE DERIVATIVES AND METHODS OF USE THEREOF
    1.
    发明申请
    4-AMINOQUINAZOLINE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
    4-氨基喹啉衍生物及其使用方法

    公开(公告)号:WO2008024439A3

    公开(公告)日:2009-02-26

    申请号:PCT/US2007018655

    申请日:2007-08-22

    发明人: TUNG ROGER

    CPC分类号: C07D405/04

    摘要: This invention relates to novel 4-aminoquinazolines, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the EGFR and HER-2.

    摘要翻译: 本发明涉及新的4-氨基喹唑啉,其衍生物,药学上可接受的盐,溶剂合物和水合物。 本发明还提供包含本发明化合物的组合物和这些组合物在治疗通过施用EGFR和HER-2抑制剂有益治疗的疾病和病症的方法中的用途。

    AN IMPROVED ONE POT PROCESS FOR MAKING KEY INTERMEDIATE FOR GEMCITABINE HCL
    4.
    发明申请
    AN IMPROVED ONE POT PROCESS FOR MAKING KEY INTERMEDIATE FOR GEMCITABINE HCL 审中-公开
    改进的一个方法,用于制备化学药物HCL的关键中间体

    公开(公告)号:WO2007049295B1

    公开(公告)日:2007-08-30

    申请号:PCT/IN2006000219

    申请日:2006-06-27

    IPC分类号: C07D307/26

    CPC分类号: C07D405/04 C07H19/073

    摘要: An improved one pot process for preparing 2-deoxy-D-erythro-2,2-difluoro-pentafuranose-1-ulose-3,5-dibenzoate of Formula (I) comprising hydrolysis of (erythro:threo) alkyl-3-dioxalan-4-yl-2,2-difluoro-3-hydroxy propionate of Formula (III) where alkyl group is having C1-C4 number of carbon atoms using a mild acid and selectively isolating 2-deoxy-D-erythro-2,2-difluoro-pentafuranose-1-ulose-3,5-dibenzoate from the mixture of erythro & threo enantiomers using ethyl acetate, ethylene dichloride and diisopropyl ether as solvents with improved yield and purity.

    摘要翻译: 一种改进的一锅法制备式(I)的2-脱氧-D-赤式-2,2-二氟 - 五呋喃糖-1-尿苷-3,5-二苯甲酸酯,其包括(赤式:苏式)烷基-3-二恶烷 (III)的4-基-2,2-二氟-3-羟基丙酸酯,其中烷基使用温和酸具有C 1 -C 4数目的碳原子,并选择性分离2-脱氧-D-赤式-2,2 使用乙酸乙酯,二氯乙烷和二异丙基醚作为溶剂,从提供的产率和纯度得到来自赤皂苷和苏糖对映异构体的混合物的二氟 - 五氟烷基-1-尿苷-3,5-二苯甲酸酯。

    METHOD FOR THE PREPARATION OF CITALOPRAM
    6.
    发明申请
    METHOD FOR THE PREPARATION OF CITALOPRAM 审中-公开
    方法制备CITALOPRAM

    公开(公告)号:WO01047909A1

    公开(公告)日:2001-07-05

    申请号:PCT/DK1999/000739

    申请日:1999-12-28

    摘要: The present invention relates to a method for the preparation of citalopram or any of its enantiomers and acid addition salts thereof comprising reaction of a compound of formula (II), with a diene having formula (III), wherein X is O, S, SO2, -N=N-, -CO-O-, -O-CO-, or with a diene having formula (IV) wherein R is alkyl or optionally substituted aryl or arylalkyl. The invention also relates to intermediates used in the new process for the preparation of citalopram, as well as citalopram prepared according to the new process.

    摘要翻译: 本发明涉及一种制备西酞普兰或其任何对映异构体及其酸加成盐的方法,其包括式(II)化合物与式(III)的二烯反应,其中X为O,S,SO 2 ,-N = N-,-CO-O-,-O-CO-或具有式(Ⅳ)的二烯,其中R是烷基或任意取代的芳基或芳烷基。 本发明还涉及用于制备西酞普兰的新方法的中间体以及根据新方法制备的西酞普兰。