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    • 79. 发明授权
    • Arylperfluoroalkanes
    • 芳基全氟烷烃
    • US4071570A
    • 1978-01-31
    • US659624
    • 1976-02-20
    • Edward L. EngelhardtMarcia E. Christy
    • Edward L. EngelhardtMarcia E. Christy
    • C07C17/00C07C17/14C07C17/16C07C17/18C07C25/18C07C29/147C07C33/46C07C45/00C07C45/28C07C45/51C07C45/52C07C45/63C07C45/64C07C45/78C07C49/807C07C49/813C07C49/84C07C63/70C07D233/20C07C25/00
    • C07D233/20C07C17/14C07C17/16C07C17/18C07C17/392C07C25/18C07C29/147C07C33/46C07C45/004C07C45/28C07C45/51C07C45/513C07C45/52C07C45/63C07C45/64C07C45/78Y10S514/821
    • 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.
    • 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。