An unexpected isomerization of azomethine ylides generated in situ from isatin with indoline-2-carboxylic acid has been disclosed, providing direct access to N-functionalized indole scaffolds. This protocol has good functional group tolerance and provides various 3-(1H-indol-1-yl)indolin-2-one derivatives in moderate to high yields simply by using alcohol as the solvent, with no additional additive
5-HETEROARYLINDOLE DERIVATIVES AS BENZODIAZEPINE RECEPTOR SITE AGONISTS AND ANTAGONISTS
申请人:PFIZER INC.
公开号:EP0743942A1
公开(公告)日:1996-11-27
[EN] 5-HETEROARYLINDOLE DERIVATIVES AS BENZODIAZEPINE RECEPTOR SITE AGONISTS AND ANTAGONISTS<br/>[FR] DERIVES DE 5-HETEROARYLINDOLE UTILISES COMME AGONISTES ET ANTAGONISTES DU SITE RECEPTEUR DE LA BENZODIAZEPINE
申请人:PFIZER INC.
公开号:WO1995021836A1
公开(公告)日:1995-08-17
(EN) The present invention relates to compounds of formula (I). The present invention also relates to intermediates for the preparation of compounds of formula (I), pharmaceutical compositions and method of use.(FR) La présente invention se rapporte à des composés de formule (I). On décrit également des intermédiaires destinés à la préparation des composés de formule (I), des compositions pharmaceutiques ainsi qu'un procédé d'utilisation de ces composés.
Ishii, Hisashi; Sakurada(nee Kawanabe), Eri; Murakami, Keiko, Journal of the Chemical Society. Perkin transactions I, 1988, p. 2387 - 2396