Arylperfluoroalkanes
    7.
    发明授权
    Arylperfluoroalkanes 失效
    芳基全氟烷烃

    公开(公告)号:US4071570A

    公开(公告)日:1978-01-31

    申请号:US659624

    申请日:1976-02-20

    摘要: New fluoro derivatives of aralkylamine compounds, particularly 2-(2-phenyl-1,1,2,2-tetrafluoroethyl)benzylamine, as well as the N-alkyl and the N,N-dialkyl derivatives thereof are prepared by reaction of 2-bromobenzonitrile with benzylmagnesium chloride to produce 2'-bromo-2-phenylacetophenone; oxidation of said acetophenone with selenous acid to produce 2-bromobenzil; conversion of the benzil compound by treatment with sulfur tetrafluoride to the corresponding 2-bromo-.alpha.,.alpha.-.alpha.',.alpha.'-tetrafluorobibenzyl;followed by reaction of the 2-bromobibenzyl compound with a metal cyanide to produce the corresponding 2-(2-phenyl-1,1,2,2-tetrafluoroethyl)benzonitrile. This nitrile compound is then reduced with lithium aluminum hydride to produce the corresponding benzylamine, which is then converted, if desired, to the N-alkyl and/or N,N-dialkyl 2-(2-phenyl-1,1,2,2-tetrafluoroethyl)benzylamine. Alternatively, the nitrile or the precursor bromobibenzyl can be converted by Grignard reactions to the corresponding .alpha.-alkyl or .alpha.,.alpha.-dialkylbenzylamine which can then be converted if desired to the corresponding N-alkyl and/or N,N-dialkyl substituted benzylamine compound. The phenyltetrafluoroethylbenzylamine as well as its N-alkyl and N,N-dialkyl derivatives are active as antiarrhythmic agents.

    摘要翻译: 芳烷基胺化合物,特别是2-(2-苯基-1,1,2,2-四氟乙基)苄胺以及N-烷基和N,N-二烷基衍生物的新的氟衍生物通过2- 溴苄腈与苄基氯化镁反应生成2'-溴-2-苯基苯乙酮; 用硒酸氧化所述苯乙酮以产生2-溴苯甲醇; 通过用四氟化硫处理将苯偶酰化合物转化成相应的2-溴-α,α-α',α'-四氟联苄;然后将2-溴苄基化合物与金属氰化物反应,生成相应的2-(2 苯基-1,1,2,2-四氟乙基)苄腈。 然后将该腈化合物用氢化铝锂还原以产生相应的苄胺,然后如果需要将其转化为N-烷基和/或N,N-二烷基2-(2-苯基-1,1,2, 2-四氟乙基)苄胺。 或者,腈或前体溴联苄可以通过格利雅反应转化成相应的α-烷基或α,α-二烷基苄基胺,如果需要,可以将其转化成相应的N-烷基和/或N,N-二烷基取代的苄胺化合物 。 苯基四氟乙基苄胺以及其N-烷基和N,N-二烷基衍生物作为抗心律不齐剂是有活性的。

    4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-methylpiperidine-N-oxide
isomer
    8.
    发明授权
    4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-methylpiperidine-N-oxide isomer 失效
    4-(5H-二苯并{8a,d {9环庚烯-5-亚基)-1-甲基哌啶-N-氧化物异构体

    公开(公告)号:US3992547A

    公开(公告)日:1976-11-16

    申请号:US525324

    申请日:1974-11-20

    申请人: Marcia E. Christy

    发明人: Marcia E. Christy

    IPC分类号: C07D211/94 C07D211/70

    CPC分类号: C07D211/94

    摘要: A specified geometrical isomer of 4-(5H-dibenzo-[a,d]cyclohepten-5-ylidene)-1-methylpiperidine-N-oxide is disclosed to have pharmaceutical utility as an appetite stimulant. Also disclosed are processes for the preparation of such compound; pharmaceutical compositions comprising such compound; and methods of treatment comprising administering such compound and compositions.

    摘要翻译: 公开了4-(5H-二苯并 - [a,d]环庚烯-5-亚基)-1-甲基哌啶-N-氧化物的特定几何异构体作为食欲刺激剂具有药物效用。 还公开了制备这种化合物的方法; 包含该化合物的药物组合物; 和治疗方法,包括施用这种化合物和组合物。