Bicyclic tetrahydrofuran lactone derivatives and process for the preparation thereof
    1.
    发明申请
    Bicyclic tetrahydrofuran lactone derivatives and process for the preparation thereof 失效
    双环四氢呋喃内酯衍生物及其制备方法

    公开(公告)号:US20070010679A1

    公开(公告)日:2007-01-11

    申请号:US11303125

    申请日:2005-12-15

    IPC分类号: C07D493/02

    CPC分类号: C07D493/02

    摘要: The present invention relates to bicyclic tetrahydrofuran lactone derivatives of Formula (1) and a preparation method thereof, and particularly it relates to a process of preparing compounds of Formula (1) by performing an intramolecular cyclization of tetrahydrofuran-allenic acid derivatives in the presence of a phenyl halide, a palladium catalyst and a base: wherein n is 1 or 2, and R is phenyl optionally substituted with C1-C6 alkyl, C1-C6 alkoxy, hydroxyl or C1-C6 hydroxyalkyl group.

    摘要翻译: 本发明涉及式(1)的双环四氢呋喃内酯衍生物及其制备方法,特别涉及通过在四氢呋喃 - 异丙酸衍生物的存在下进行分子内环化制备式(1)化合物的方法, 苯基卤化物,钯催化剂和碱:其中n为1或2,R为任选被C 1 -C 6烷基取代的苯基,C 1 -C 6烷基, C 1 -C 6烷氧基,羟基或C 1 -C 6羟烷基。

    Synthesis of 7-membered carbocyclic compound having diexomethylene groups
    3.
    发明申请
    Synthesis of 7-membered carbocyclic compound having diexomethylene groups 失效
    具有阴离子亚甲基的7-元碳环化合物的合成

    公开(公告)号:US20050059832A1

    公开(公告)日:2005-03-17

    申请号:US10823707

    申请日:2004-04-14

    CPC分类号: C07D493/08

    摘要: The present invention relates to a synthesis of a 7-membered carbocyclic compound having diexomethylene groups, more particularly to a synthesis of a 7-membered carbocyclic compound having diexomethylene groups, a novel compound having the structure represented by the following Chemical Formula 1, from trimethylsilanylmethyl-allenol derivative by the intramolecular Prins cyclization using Lewis acid. The 7-membered carbocyclic compound is a useful intermediate for synthesis of other multicyclic compounds. In Chemical Formula 1, R1 is a C1 to C6 alkyl group, and R2 and R3 is respectively a hydrogen atom, or R1, R2 and R3 may be connected with neighboring substituents to form a 5 to 10-membered aliphatic or aromatic ring.

    摘要翻译: 本发明涉及具有阴离子亚甲基的7-元碳环化合物的合成,更具体地说,涉及具有下式化学式1所示结构的新化合物,具有三亚甲基硅烷基甲基的三元碳环化合物 通过使用路易斯酸的分子内Prins环化形成的α-烯醇衍生物。 7元碳环化合物是合成其他多环化合物的有用中间体。 在化学式1中,R 1是C 1 -C 6烷基,R 2和R 3分别是氢原子,或者R 1,R 2和R 3可以是 与相邻取代基连接形成5至10元脂族或芳环。

    SYNTHESIS OF 8-MEMBERED CARBOCYCLIC COMPOUND HAVING DIEXOMETHYLENE GROUPS
    4.
    发明申请
    SYNTHESIS OF 8-MEMBERED CARBOCYCLIC COMPOUND HAVING DIEXOMETHYLENE GROUPS 失效
    具有二甲苯基组合物的8组分碳化合物的合成

    公开(公告)号:US20050059732A1

    公开(公告)日:2005-03-17

    申请号:US10823708

    申请日:2004-04-14

    CPC分类号: C07D493/08 A61K31/343

    摘要: The present invention relates to a synthesis of an 8-membered carbocyclic compound having diexomethylene groups, more particularly to a synthesis of an 8-membered carbocyclic compound having diexomethylene groups, a novel compound having the structure represented by the following Chemical Formula 1, from trimethylsilanylmethyl-allenol derivative by the intramolecular Prins cyclization using Lewis acid. The 8-membered carbocyclic compound is a useful intermediate for synthesis of other multicarbocyclic compounds. In Chemical Formula 1, R1 is a phenyl group, and R2 and R3 is a hydrogen atom, or R1, R2 and R3 may be connected with neighboring substituents to form a 5 to 10-membered aliphatic or aromatic ring.

    摘要翻译: 本发明涉及具有阴离子亚甲基的8-元碳环化合物的合成,更具体地说,涉及一种具有下式化学式1所示结构的新化合物,具有三亚甲基硅烷基甲基 通过使用路易斯酸的分子内Prins环化形成的α-烯醇衍生物。 8元碳环化合物是合成其它多碳环化合物的有用中间体。 在化学式1中,R 1是苯基,R 2和R 3是氢原子,或者R 1,R 2和R 3可以与相邻的取代基连接 以形成5至10元脂族或芳族环。

    Piperazinylalkylpyrazole derivatives useful as selective T-type calcium channel blockers and preparation method thereof
    5.
    发明申请
    Piperazinylalkylpyrazole derivatives useful as selective T-type calcium channel blockers and preparation method thereof 失效
    可用作选择性T型钙通道阻滞剂的哌嗪基烷基吡唑衍生物及其制备方法

    公开(公告)号:US20070049604A1

    公开(公告)日:2007-03-01

    申请号:US11509769

    申请日:2006-08-25

    IPC分类号: A61K31/496 C07D403/02

    CPC分类号: C07D231/12 C07D405/04

    摘要: The present invention provides for novel piperazinylalkylpyrazole derivatives, the preparation method thereof and the selective T-type calcium channel blocking activity thereof. Particularly, it provides a piperazinylalkylpyrazole derivative as represented by the formula set forth below or its pharmaceutically acceptable salts, and its preparation method thereof. The compound of Formula 1 is a novel piperazinylalkylpyrazole derivative, which particulary has T-type Ca2+ channel blocking effect and thus can be useful as a therapeutic agent for nerve and muscle pain.

    摘要翻译: 本发明提供新的哌嗪基烷基吡唑衍生物,其制备方法和选择性T型钙通道阻断活性。 特别地,其提供如下式所示的哌嗪基烷基吡唑衍生物或其药学上可接受的盐及其制备方法。 式1的化合物是新型的哌嗪基烷基吡唑衍生物,特别是具有T型Ca 2+通道阻断效应,因此可用作神经和肌肉疼痛的治疗剂。

    Heterodimeric conjugates of neomycin-oxazolidinone, their preparation and their use
    6.
    发明申请
    Heterodimeric conjugates of neomycin-oxazolidinone, their preparation and their use 审中-公开
    新霉素 - 恶唑烷酮的异二聚体共轭物,其制备及其应用

    公开(公告)号:US20050222055A1

    公开(公告)日:2005-10-06

    申请号:US10502539

    申请日:2002-07-04

    CPC分类号: C07H15/232

    摘要: The present invention relates to novel oxazolidinone derivatives represented as following compound I and a process for the preparation thereof. The compounds of the present invention have wide antibacterial spectrums superior antibacterial activity and low toxicity. Therefore, it can be expected to use as novel antibacterial agent. wherein, R1 is alkylcarboxyl group or —CH2R2 (wherein, R2 is OH, argido group, —OR3 (wherein, R3 is C1-4 alkyl, methansulfonyl, p-toluensulfonyl, carboxyl, C1-4 alkylcarboxyl, C1-4 alkylcarbonyl, benzyloxycarbonyl, or imidazolylcarbonyl), or —NHR4).

    摘要翻译: 本发明涉及以下述化合物I表示的新型恶唑烷酮衍生物及其制备方法。 本发明的化合物具有广泛的抗菌谱,抗菌活性和毒性低。 因此,可以预期用作新型抗菌剂。 其中R 1是烷基羧基或-CH 2 R 2 R 2(其中R 2是OH,argido 基团,-OR 3(其中R 3是C 1-4烷基,甲磺酰基,对甲苯磺酰基,羧基,C 1 -C 4烷基, 1-4烷基羧基,C 1-4烷基羰基,苄氧基羰基或咪唑基羰基)或-NHR 4)。