Process for the manufacture of racemic (R,R; S,S) asocainol
    25.
    发明授权
    Process for the manufacture of racemic (R,R; S,S) asocainol 失效
    用于制备外消旋(R,R; S,S)asocainol的方法

    公开(公告)号:US4649196A

    公开(公告)日:1987-03-10

    申请号:US730124

    申请日:1985-05-03

    CPC分类号: C07D225/08

    摘要: A process for the preparation of racemic asocainol in the (R,R; S,S)-form and (-)-asocainol in the (S,S)-form as well as the pharmacologically compatible salts thereof is herein described on the basis of a thermal rearrangement of the inactive (R,S)-diastereomer to the (S,S)-form.Racemic (.+-.)-asocainol and the (-)-enantiomer are potent antiarrhythmic agents and local anesthetics.

    摘要翻译: 在(S,S)形式的(R,R; S,S)形式和( - ) - 焦氨醇中制备外消旋asocainol以及其药理学上相容的盐的方法在此基于 的非活性(R,S) - 非对映体与(S,S) - 形式的热重排。 外消旋(+/-) - asocainol和( - ) - 对映异构体是有效的抗心律失常药和局部麻醉药。

    Benzo(b)thiophene derivatives
    27.
    发明授权
    Benzo(b)thiophene derivatives 失效
    BENZO(B)噻吩衍生物

    公开(公告)号:US4056526A

    公开(公告)日:1977-11-01

    申请号:US691109

    申请日:1976-05-28

    IPC分类号: C07D413/04 C07D413/02

    CPC分类号: C07D413/04

    摘要: The present invention relates to novel benzo(b)thiophene derivatives of the general formula: ##STR1## wherein Y represents a hydrogen or halogen atom; A represents a hydrogen atom or a phenyl group which may be substituted with a halogen atom or a lower alkoxy group; B represents a radical of the formula OR' or NR.sup.2 R.sup.3, wherein R' is an alkyl radical of 1 to 5 carbons which may be substituted with hydroxy, lower alkoxy, phenyl or phenoxy groups or a cycloalkyl or phenyl group which may be substituted by lower alkoxy or halogen atoms; R.sup.2 and R.sup.3, which may be identical or different, represent, if identical, hydrogen, alkyl radicals of 1 to 5 carbon atoms which may be substituted by hydroxy, lower alkoxy, phenoxy, di-lower alkylamino, or phenyl groups; or, if R.sup.2 is hydrogen, R.sup.3 represents either a hydroxyl or an amino group which may be substituted by lower alkyl, dialkyl, alkylidene, phenyl or acyl groups or a lower alkyl group which may be substituted by hydroxy, lower alkoxy, phenoxy, dialkylamino, pyrrolidino, piperidino or morpholino groups; R.sup.3 further is a cycloalkyl or phenyl group, which may be substituted by a halogen or a lower alkoxy radical; or R.sup.2 and R.sup.3 together with the nitrogen atom to which they are attached, may form an aziridine, pyrrolidine, piperidine, morpholine or piperazine ring which may be substituted by lower alkyl, hydroxyalkyl, phenylalkyl, phenyl or acetyl groups; or A and B together with the C.dbd.N group may form a 5, 6, or 7-membered heterocyclic ring.

    Process for the preparation of 1-(m- and p-hydroxyphenyl)-2-aminoethanol
    29.
    发明授权
    Process for the preparation of 1-(m- and p-hydroxyphenyl)-2-aminoethanol 失效
    制备1-(间 - 和对羟基苯基)-2-氨基乙醇的方法

    公开(公告)号:US3966813A

    公开(公告)日:1976-06-29

    申请号:US264698

    申请日:1972-06-20

    IPC分类号: C07C85/11

    CPC分类号: C07C2101/14

    摘要: The present invention relates to a process for the preparation of 1-(m- and p- hydroxyphenyl)-2-aminoethanol which consists of converting an m- or p- hydroxyacetophenone to an isonitrosoketone followed by hydrogenation of the isonitrosoketone. These compounds are sympathomimetics which produce vasoconstricting and cardiotonic effects.

    摘要翻译: 本发明涉及一种制备1-(间 - 和对羟基苯基)-2-氨基乙醇的方法,其由将对羟基苯乙酮或对羟基苯乙酮转化为异亚硝基酮,然后氢化异硝基酮而组成。 这些化合物是产生血管收缩和强心作用的交感神经瘤。