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    2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazines
    1.
    发明授权
    2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazines 失效
    2-（3-取代的氨基-2-羟基丙氧基）-3-取代的吡嗪

    公开(公告)号：US3946009A

    公开(公告)日：1976-03-23

    申请号：US408032

    申请日：1973-10-19

    申请人： Burton Kendall Wasson ,  Leonard M. Weinstock

    发明人： Burton Kendall Wasson ,  Leonard M. Weinstock

    IPC分类号： C07D241/18 ,  C07D413/04 ,  C07D295/00

    CPC分类号： C07D413/04 ,  C07D241/18 ,  Y10S514/821

    摘要： 2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazine compounds optionally having substituents in the 5 and/or 6 positions, possessing .beta.-adrenergic blocking properties are described. The products are prepared by reaction of a 2-chloro(or hydroxy)pyrazine with a 5-hydroxy-methyl(or sulfonyloxymethyl)oxazolidine followed by acid hydrolysis.

    摘要翻译： 描述了具有β-肾上腺素能阻断性质的5-和/或6位任选具有取代基的2-（3-取代的氨基-2-羟基丙氧基）-3-取代的吡嗪化合物。 产物通过2-氯（或羟基）吡嗪与5-羟基 - 甲基（或磺酰氧基甲基）恶唑烷的反应然后酸水解反应制备。

    1,8-Naphthyridine compounds
    3.
    发明授权
    1,8-Naphthyridine compounds 失效
    1,8-萘啶化合物

    公开(公告)号：US3993656A

    公开(公告)日：1976-11-23

    申请号：US551565

    申请日：1975-02-20

    申请人： Clarence Stanley Rooney ,  Haydn Windsor Richard Williams ,  Burton Kendall Wasson

    发明人： Clarence Stanley Rooney ,  Haydn Windsor Richard Williams ,  Burton Kendall Wasson

    IPC分类号： C07C45/45 ,  C07C49/167 ,  C07D209/12 ,  C07D209/14 ,  C07D213/87 ,  C07D233/54 ,  C07D471/04 ,  C07F5/02

    CPC分类号： C07D213/87 ,  C07C45/455 ,  C07C49/167 ,  C07D209/12 ,  C07D209/14 ,  C07D233/64 ,  C07D471/04 ,  C07F5/022

    摘要： There is described 1,8-naphthyridin-2(1H)-one compounds with bronchodilating and hypotensive properties prepared by reaction of 2,6-diaminopyridine with an appropriate .beta.-diketone providing a 2-aminonaphthyridine compound which upon treatment with nitrous acid is converted to the 2-oxo product. Alternatively, an appropriate .beta.-diketone can be reacted with an alkyl alkoxycarbonylacetimidate, the alkyl 2-aminonicotinate thus formed converted to the hydrazide, which upon treatment with a sulfonyl halide forms the N-sulfonyl hydrazide derivative. This intermediate is reacted with an alkali metal carbonate to provide the 2-aminonicotinaldehyde which upon reaction with an ester of a substituted aliphatic carboxylic acid provides the desired product. In some cases the aminonicotinaldehyde is generated in situ in the presence of the ester thereby giving the desired product in one step from the N-sulfonyl hydrazide derivative.

    摘要翻译： 描述了通过2,6-二氨基吡啶与合适的β-二酮反应制备的支气管扩张和降血压特性的1,8-萘啶-2（1H） - 酮化合物，其提供2-氨基萘啶化合物，其在用亚硝酸处理时被转化 与2-氧代产物。 或者，合适的β-二酮可以与烷基烷氧基羰基亚酰亚胺酯反应，由此形成的2-氨基烟酸烷基酯转化成酰肼，其在用磺酰卤处理时形成N-磺酰肼衍生物。 该中间体与碱金属碳酸盐反应以提供2-取代的脂肪族羧酸的酯与提供所需产物反应的2-氨基二醛。 在一些情况下，在酯存在下原位产生氨基烟醛，从而从N-磺酰肼衍生物一步得到所需产物。

    4-(3-Amino-2-acyloxypropoxy)-1,2,5-thiadiazole compounds
    4.
    发明授权
    4-(3-Amino-2-acyloxypropoxy)-1,2,5-thiadiazole compounds 失效
    4-（3-氨基-2-氰基丙基）-1,2,5-噻二唑化合物

    公开(公告)号：US4011217A

    公开(公告)日：1977-03-08

    申请号：US553186

    申请日：1975-02-26

    申请人： Burton Kendall Wasson

    发明人： Burton Kendall Wasson

    IPC分类号： C07D285/10 ,  C07D295/12

    CPC分类号： C07D285/10

    摘要： 4-[3-(Substituted amino)-2-acyloxypropoxy]-1,2,5-thiadiazole compounds, optionally substituted in the 3-position of the thiadiazole nucleus which exhibit .beta.-adrenergic blocking properties and thus are useful in the management of angina pectoris are described. The products are prepared by reaction of a 4-[3-(substituted amino)-2-hydroxypropoxy]-1,2,5-thiadiazole with the appropriate anhydride. The reaction is run under acidic conditions when the amino nitrogen is protonated.