Process for producing (8-chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-B]pyridin-11-YL)-1-piperdine
    86.
    发明授权
    Process for producing (8-chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-B]pyridin-11-YL)-1-piperdine 失效
    (8-氯-3,10-二溴-6,11-二氢-5H-苯并[5,6]环庚并[1,2-B]吡啶-11-YL)-1-哌啶的制备方法

    公开(公告)号:US06706883B1

    公开(公告)日:2004-03-16

    申请号:US09345966

    申请日:1999-07-01

    IPC分类号: C07D40104

    CPC分类号: C07D401/04

    摘要: A process for producing compounds of the formula: is disclosed. The compound of formula 1.0 is produced by: (1) separating the atropisomers of  to obtain the atropisomers (2) heating the atropisomer of formula 2.0B at a suitable temperature in a suitable solvent to obtain a mixture of atropisomers of formulas 2.0A and 2.0B; (3) separating the atropisomers of formulas 2.0A and 2.0B of step (2); and (4) reducing the atropisomer of formula 2.0A to obtain a compound of formula 1.0. Preferably, R1 is Br, R2 is Cl and R3 is Br. Also disclosed is the (+)-atropisomer of formula 2.0 wherein R1 is Br, R2 is Cl and R3 is Br.

    摘要翻译: 公开了一种制备下式化合物的方法。 通过以下方法制备式1.0化合物:(1)分离得到阻转异构体的阻转异构体(2)在合适的溶剂中,在合适的温度下加热式2.0B的阻转异构体,得到式2.0A和2.0B的阻转异构体的混合物 ; (3)分离步骤(2)的式2.0A和2.0B的阻转异构体; 和(4)还原式2.0A的阻转异构体以获得式1.0化合物。 优选地,R 1是Br,R 2是Cl,R 3是Br。还公开了式2.0的(+) - 阻转异构体,其中R 1是Br,R 2是Cl,和 R 3是Br。

    Tri- and tetra-substituted-oxetanes and tetrahydrofurans and
intermediates thereof
    89.
    发明授权
    Tri- and tetra-substituted-oxetanes and tetrahydrofurans and intermediates thereof 失效
    三取代 - 氧杂环丁烷和四氢呋喃及其中间体

    公开(公告)号:US5039676A

    公开(公告)日:1991-08-13

    申请号:US460342

    申请日:1990-05-11

    摘要: This invention relates to tri- and tetra-substituted-oxetanes, e.g. (.+-.)-cis- and (.+-.)-trans-2-[(4-(4-isopropylpiperazin-1-yl)phenoxy)methyl]-4-(2,4-dihalophenyl)-4-[1H-1,2,4-triazol-1-yl)-methyl]oxetane and tri- and tetra-substituted-tetrahydrofurans, e.g. (.+-.)-cis- and (.+-.)-trans-1-[4-[[2-(2,4-dihalophenyl)tetrahydro-2-[(1H-azol-1-yl)methyl]-5-furanylmethoxy]phenyl]-4-yl-1-substituted piperazine-3-one and related derivatives which exhibit antifungal and antiallergy activities, pharmaceutical composition thereof, methods of their use in treating or preventing susceptible fungal infections and allergic reactions in a host including warm-blooded animals such as humans.

    摘要翻译: 本发明涉及三 - 和四 - 取代 - 氧杂环丁烷,例如 (+/-) - 顺式 - 和(+/-) - 反式-2 - [(4-(4-异丙基哌嗪-1-基)苯氧基)甲基] -4-(2,4-二卤代苯基) [1H-1,2,4-三唑-1-基] - 甲基]氧杂环丁烷和三取代 - 四氢呋喃,例如 (+/-) - 顺 - 和(+/-) - 反式-1- [4 - [[2-(2,4-二卤苯基)四氢-2 - [(1H-氮杂-1-基)甲基] -5-呋喃基甲氧基]苯基] -4-基-1-取代的哌嗪-3-酮及其相关衍生物,其具有抗真菌和抗过敏活性,其药物组合物,其用于治疗或预防易感性真菌感染和其中的过敏反应的方法 宿主包括温血动物如人类。