Development of a Modified Julia Olefination of Imides for the Synthesis of Alkaloids
作者:Huu Vinh Trinh、Lionel Perrin、Peter G. Goekjian、David Gueyrard
DOI:10.1002/ejoc.201600349
日期:2016.6
We report the development of the intramolecular Juliaolefination of imides. This original reaction produces N-fused bicyclic enamide compounds, which are interesting precursors in the synthesis of alkaloids. We show that this transformation enables access to [5,6], [6,5], and [6,6] fused bicyclic lactam enamides. The scope and the limitations of the reaction are presented as well as computational
我们报告了酰亚胺的分子内 Julia 烯化的发展。这种原始反应产生 N-稠合双环烯酰胺化合物,它们是生物碱合成中有趣的前体。我们表明,这种转化能够获得 [5,6]、[6,5] 和 [6,6] 稠合双环内酰胺烯酰胺。介绍了反应的范围和局限性,以及有关标题反应新机理方面的计算研究。
Compounds having the formula ##STR1## wherein A is a straight or branched chain alkylene group; R is hydrogen, halogen, alkyl, alkoxy, alkylthio, trifluoromethyl, nitro, amino, or cyano; and m is 2, 3 or 4; are useful in the treatment of allergic conditions in mammals.
Compounds having the formula ##STR1## wherein A is a straight or branched chain alkylene group; R.sub.1 is hydrogen, halogen, alkyl, alkoxy, alkylthio, trifluoromethyl, nitro, amino, or cyano; and n is 0, 1, or 2; are useful central nervous system depressants.
A series of piperazinopyrrolo[1,2-a]thieno[3,2-e]pyrazinederivatives were prepared and evaluated to determine their affinity for the 5-HT7 receptor. Various substitutions on piperazine were explored as well as replacement of the piperazine by other amines.
Hexahydro-trans- and tetrahydropyridoindole neuroleptic agents
申请人:PFIZER INC.
公开号:EP0060610A1
公开(公告)日:1982-09-22
Derivatives of 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole and of (+)enantiomeric, mixtures of (+) and (-)-enantiomeric or (±)racemic 2,3,4,4a,5,9b-hexahydro-4a, 9b-trans-1H-pyrido[4,3-b]indole, substituted at the 5-position with an aryl group and at the 2-position with a carbonylaminoalkyl group or an aminoalkyl group, are neuroleptic agents useful in the treatment of certain psychoses and neuroses.