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    Optically active isocarbostyril derivatives and a method of preparing the same
    2.
    发明授权
    Optically active isocarbostyril derivatives and a method of preparing the same 失效
    光活性异卡波斯特尔衍生物及其制备方法

    公开(公告)号：US4659833A

    公开(公告)日：1987-04-21

    申请号：US731963

    申请日：1985-05-08

    申请人： Toshihiro Takahashi ,  Noriyoshi Sueda ,  Masahiro Tsuji ,  Yoshiyuki Tahara ,  Hiroyasu Koyama ,  Yoshikuni Suzuki ,  Masao Nagase ,  Toshiji Sugai

    发明人： Toshihiro Takahashi ,  Noriyoshi Sueda ,  Masahiro Tsuji ,  Yoshiyuki Tahara ,  Hiroyasu Koyama ,  Yoshikuni Suzuki ,  Masao Nagase ,  Toshiji Sugai

    IPC分类号： C07D215/56 ,  A61K31/47 ,  A61K31/472 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  C07D209/48 ,  C07D209/49 ,  C07D217/24 ,  C07D405/12 ,  C07D413/12

    CPC分类号： C07D413/12 ,  C07D217/24

    摘要： Four different optical isomers of a new compound, 1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4"-isocarbostyriloxy)-2-propanol are now provided as new substances. These four optical isomers are now named as (2R, 1'S)-1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4"-isocarbostyriloxy)-2-propanol, (2S, 1'S)-1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4"-isocarbostyriloxy)-2-propanol, (2S, 1'R)-1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4"-isocarbostyriloxy)-2-propanol, and (2R, 1'R)-1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4"-isocarbostyriloxy)-2-propanol, respectively. These four optical isomers have different activities for their .beta.-adrenergic-blocking effect and .alpha.-adrenergic-blocking effect and are useful as valuable agents for therapeutic treatment of various cardiovascular diseases, as compared to an optically inactive racemic mixture of said isomer compounds. These four optical isomers may be produced and isolated from each other by chromatographing (1'S)- or (1'R)-N-[2'-(o-methoxyphenoxy)-1'-methylethyl]-5-(4"-isocarbostyriloxymethyl)-2-oxazolidones to isolate either its (5R, 1'S)-isomer and its (5S, 1'S)-isomer, or its (5S, 1'R)-isomer and its (5R, 1'R)-isomer therefrom separately and then hydrolyzing each of these isolated isomers under alkaline conditions to obtain separately (2R, 1'S)-, (2S, 1'S)-, (2S, 1'R)- and (2R, 1'R)-1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4"-isocarbostyriloxy)-2-propanols.

    摘要翻译： 现在提供新的化合物1- [2' - （邻甲氧基苯氧基）-1'-甲基乙基氨基] -3-（4“ - 异卡波酰氧基）-2-丙醇的四种不同的光学异构体作为新物质。 这些四种光学异构体现在命名为（2R，1'S）-1- [2' - （邻甲氧基苯氧基）-1'-甲基乙基氨基] -3-（4“ - 异卡波铵氧基）-2-丙醇，（2S， 1'S）-1- [2' - （邻甲氧基苯氧基）-1'-甲基乙基氨基] -3-（4“ - 异卡波铵氧基）-2-丙醇，（2S，1'R）-1- [ （邻甲氧基苯氧基）-1'-甲基乙基氨基] -3-（4“ - 异卡波铵氧基）-2-丙醇和（2R，1'R）-1- [2' - （邻甲氧基苯氧基） - 甲基乙基氨基] -3-（4“ - 异卡波铵氧基）-2-丙醇。 与所述异构体化合物的光学上无活性的外消旋混合物相比，这四种光学异构体对于β-肾上腺素能阻滞效应和α-肾上腺素能阻断效应具有不同的活性，并且可用作治疗各种心血管疾病的有价值的药剂。 这些四种光学异构体可以通过色谱法（1'S） - 或（1'R）-N- [2' - （邻甲氧基苯氧基）-1'-甲基乙基] -5-（4“ - （5R，1'S） - 异构体或其（5S，1'R） - 异构体及其（5R，1'R） - 异构体 然后分别在碱性条件下水解这些分离的异构体，分别得到（2R，1'S） - ，（2S，1'S） - ，（2S，1'R） - 和（2R，1'R）-1- [ 2' - （邻甲氧基苯氧基）-1'-甲基乙基氨基] -3-（4“ - 异卡波铵氧基）-2-丙醇。

    Optically active bicyclo[3.3.0]octane and processes for the preparation thereof
    4.
    发明授权
    Optically active bicyclo[3.3.0]octane and processes for the preparation thereof 失效
    光学活性双环[3.3.0]辛烷及其制备方法

    公开(公告)号：US4871869A

    公开(公告)日：1989-10-03

    申请号：US293414

    申请日：1989-01-04

    申请人： Kenji Mori ,  Masahiro Tsuji

    发明人： Kenji Mori ,  Masahiro Tsuji

    IPC分类号： C07C405/00 ,  C07D317/72 ,  C07F7/18

    CPC分类号： C07D317/72 ,  C07C405/0083 ,  C07F7/1856 ,  Y02P20/582

    摘要： New intermediate, an optically active (1R,5S,6S,7R)-6-tert-butyldiphenylsilyloxmethyl-7-hydroxy-bicyclo[3.3.0]octan-3-one (I) having high optical purity which is useful for the synthesis of an optically active carbacyclin and an optically active pentalenolactone E methyl ester. The compound (I) is also an intermediate compound serving for the purpose of improving the optical purity of (1R,5S,6S,7R)-3,3-ethylenedioxy-6-hydroxymethyl-7-(2'-tetrahydropyranyloxy)bicyclo[3.3.0]octane. The compound (I) is prepared by reacting (1R,5S,6S,7R)-3,3-ethylenedioxy-6-hydroxymethyl-7-(2'-tetrahydropyranyloxy)bicyclo[3.3.0]octane with tert-butylchlorodiphenylsilane in the presence of a base and removing the ethylenedioxy and tetrahydropyranyl groups of the resultant compound under an acid condition.

    High-strength, high-conductivity copper alloy
    5.
    发明授权
    High-strength, high-conductivity copper alloy 失效
    高强度，高导电性铜合金

    公开(公告)号：US4666667A

    公开(公告)日：1987-05-19

    申请号：US844237

    申请日：1986-03-25

    申请人： Morinori Kamio ,  Masahiro Tsuji ,  Hirohito Miyashita

    发明人： Morinori Kamio ,  Masahiro Tsuji ,  Hirohito Miyashita

    IPC分类号： C22C9/00 ,  C22C9/02 ,  H01B1/02

    CPC分类号： C22C9/02 ,  C22F1/08

    摘要： A high-strength, high-conductivity copper alloy comprises, all by weight, from 0.8 to 4.0% of Sn, from more than 0.01 to 0.4% of P, from 0.05 to 1.0% of Ni, from 0.05 to 1.0% of one, two or more elements selected from Al, Hf, Be, Mo, Zn, Te, Pb, Co, Zr, and Nb, and the remainder of Cu and inevitable impurities. The impurities include not more than 0.0020% of oxygen.

    摘要翻译： 高强度，高导电性铜合金全部重量含有Sn：0.8〜4.0％，P：0.01〜0.4％，Ni：0.05〜1.0％，0.05〜1.0％ 选自Al，Hf，Be，Mo，Zn，Te，Pb，Co，Zr和Nb中的两种或更多种元素，其余的Cu和不可避免的杂质。 杂质含有不大于0.0020％的氧气。

    High-strength-conductivity copper alloy
    6.
    发明授权
    High-strength-conductivity copper alloy 失效
    高强度导电铜合金

    公开(公告)号：US4362579A

    公开(公告)日：1982-12-07

    申请号：US219617

    申请日：1980-12-24

    申请人： Masahiro Tsuji

    发明人： Masahiro Tsuji

    IPC分类号： C22C9/00 ,  C22C9/04 ,  H01B1/02 ,  H01H1/025 ,  C22F1/08

    CPC分类号： C22C9/04 ,  H01H1/025

    摘要： A copper alloy with high strength and excellent electrical conductivity, corrosion resistance, and spring qualities, comprises 0.4-8% nickel, 0.1-3% silicon, 10-35% zinc, concomitant impurities, and the remainder copper, all by weight. It further comprises at least one element as an accessory ingredient or ingredients selected from the group consisting of 0.001-0.1 wt % each of phosphorus and arsenic and 0.01-1 wt % each of titanium, chromium, tin, and magnesium. The accessory ingredient or ingredients combinedly account for 0.001-2% of the total weight of the alloy composition.

    摘要翻译： 具有高强度和优异的导电性，耐腐蚀性和弹簧质量的铜合金包括0.4-8％的镍，0.1-3％的硅，10-35％的锌，伴随的杂质，其余的铜都是重量。 其还包含至少一种元素作为辅助成分或选自由磷和砷各自为0.001-0.1重量％和钛，铬，锡和镁各自为0.01-1重量％的组分组成的组分。 辅助成分或成分合成占合金组合物总重量的0.001-2％。