Substituted terphenyls
    121.
    发明授权
    Substituted terphenyls 失效
    取代的TERPHENYLS

    公开(公告)号:US3741974A

    公开(公告)日:1973-06-26

    申请号:US3741974D

    申请日:1971-03-03

    申请人: SANDOZ AG

    发明人: GRIOT R

    摘要: THIS INVENTION RELATES TO W-AMINOALKOXY SUBSTITUTED TERPHENYLS AND N-OXIDES THEREOF USEFUL AS HYPOLIPIDEMICS, AND TO PROCESSES FOR PREPARATION OF SUCH COMPOUNDS, INVOLVING KEY INTERMEDIATES WHICH INCLUDE, FOR EXAMPLE: (1) SUBSTITUTED TERCYCLIC-OLS, OR (2) P-(W - AMINOALKOXY)PHENYL DERIVATIVES OF VARIOUS COMPOUNDS WHICH ARE, FOR EXAMPLE, CYCLO-SUBSTITUTED -2-CYCLOHEXEN-1-OLS, CYCLO-SUBSTITUTED -CYCLOHEXENES OR CYCLOHEXEN-DIENES, OR (3) A-(M-TERPHENYL4-YLOXY) LOWER ALIPHATIC MONOCARBOCYCLIC ACIDS.

    3,3-disubstituted-3,4-dihydrobenzodioxepins
    122.
    发明授权
    3,3-disubstituted-3,4-dihydrobenzodioxepins 失效
    3,3-取代-3,4-二氢吲哚并[

    公开(公告)号:US3700691A

    公开(公告)日:1972-10-24

    申请号:US3700691D

    申请日:1969-06-09

    摘要: 3-Hydroxy-3-(substituted-aminoalkyl)-3,4-dihydro-2H-1,5benzodioxepin products are described that exhibit Beta adrenergic stimulating properties and are therefore suitable for use as broncho-dilating agents. The products are prepared essentially by four principal routes from 3-oxo-3,4-dihydro-2H1,5-benzodioxepins. By one route the 3-oxobenzodioxepin is treated with a nitroalkane to give a 3-hydroxy-3-nitroalkylbenzodioxepin the nitro group of which is reduced to an amine and the resulting compound reacted with an aldehyde or ketone under hydrogenating conditions to introduce the desired substituent into the amino function. By a second route the 3-oxobenzodioxepin is reacted with an alkali metal nitrile to form the cyanhydrin which upon reduction forms the 3-hydroxy-3-aminoalkylbenzodioxepin that can be treated with a ketone or aldehyde to give the desired products or can be reacted with sodium nitrite or other agent to form a 3-spiro-benzodioxepin-2''-oxirane which upon reaction with an amine provides the desired product. The 3spiro-benzodioxepin-2''-oxirane also can be obtained by treatment of the 3-oxo-benzodioxepin with a sulfurylide. A fourth method involves forming a benzodioxepin-3-spiro-5''-oxazolidin-2''-one which upon treatment with dilute alkali gives the desired 3hydroxy-3-(substituted aminoalkyl)-3,4-dihydro-2H-1,5benzodioxepin. The intermediate oxazolidinone compounds can be treated if desired with various agents to attach substituents on the benzenoid moiety of the starting substance. These oxazolidinones exhibit Beta -stimulating and skeletal muscle relaxant properties.

    摘要翻译: 描述了3-羟基-3-(取代的 - 氨基烷基)-3,4-二氢-2H-1,5-苯并二氧杂环己烯产物,其表现出β-肾上腺素能刺激性质,因此适合用作支气管扩张剂。 产物基本上由3-氧代-3,4-二氢-2H-1,5-苯并二氧杂环己酮的四条主要途径制备。 通过一条路线,用硝基烷烃处理3-氧代苯并二氧杂环己烷,得到3-硝基烷基 - 苯并二氧杂环己烯,其硝基还原成胺,所得化合物在氢化条件下与醛或酮反应,引入 所需的取代基进入氨基官能团。 通过第二种途径,3-氧代苯并二氧杂环己酮与碱金属腈反应形成氰醇,当还原形成3-羟基-3-氨基烷基 - 苯并二氧杂环己酮时,可用酮或醛处理以产生所需产物或可以 与亚硝酸钠或其他试剂反应以形成3-苯并二氧杂环庚-2-环氧乙烷,其与胺反应提供所需产物。 也可以通过用硫酰亚胺处理3-氧代 - 苯并二氧杂环庚烯来获得3-螺 - 苯并二氧杂环庚-2-2-环氧乙烷。 第四种方法包括形成苯并二氧杂环庚-3-烯-5-基 - 恶唑烷-2'-酮,当用稀碱处理时,得到所需的3-羟基-3-(取代的氨基烷基)-3,4-二氢-2H- ,5-苯并二氧杂环庚烯。 如果需要,可以用各种试剂处理中间体恶唑烷酮化合物以在起始物质的苯环部分上连接取代基。 这些恶唑烷酮表现出β-刺激和骨骼肌松弛性质。