Palladium catalyzed indolization of 2-bromo or chloroanilines

Details Palladium catalyzed indolization of 2-bromo or chloroanilines Palladium catalyzed indolization of 2-bromo or chloroanilines

C - Chemistry, Metallurgy

07

D

C07D 209/04 (2006.01)

Patent

CA 2558051

The present invention provides a method for making substituted indole compounds of general formula III comprising the step of: (a) reacting a 2- bromoaniline or 2-chloroaniline of general formula (I); wherein: X, R and R1 are defined herein with a substituted acetylene of formula (II); wherein R2 and R3 in the presence of a palladium catalyst, a ligand, and a base in a solvent at a suitable temperature to give a compound of formula (III)

La présente invention concerne un procédé permettant de produire des composés d'indole substitué de la formule générale III. Ce procédé consiste à: (a) faire réagir une 2-bromoaniline ou une 2-chloroaniline de la formule générale (I), X, R et R1 ayant la définition donnée dans la description, avec un acétylène substitué de la formule (II); R2 et R3 en présence d'un catalyseur de palladium, d'un ligand et d'une base dans un solvant à une température adéquate pour obtenir un composé de la formule (III)

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