Process for preparing substituted benzothiazinoindoles

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 513/06 (2006.01)

Patent

CA 2600271

A process for the preparation of substituted benzothiazinoindoles of general formula (I) wherein R1, R2, and R4 are independently selected from hydrogen, chloro, fluoro, amino, nitro, cyano, CHO, (C1-C3)alkyl, perhalo(Cl-C3)alkyl, (C1-C3)alkoxy, aryl, aralkyl, aralkoxy, (C5-C7)heterocyclyl, (C5- C7)heterocyclylalkyl, (C5-C7)heterocyclyloxy, acyl, acetyl, alkylamino, aminoalkyl, amide, hydroxyalkyl, carboxylic acid and its derivatives, while R3 is selected hydrogen, (C1-C3)alkyl, aryl and carboxylic acid and its derivatives is disclosed, said process comprising cyclization of compound of general formula-II, (i.e. substituted 1-benzenesulfonyl-7-bromo-lH-indole), formula (II) wherein R1, R2, R3 and R4 using suitable catalyst and solvents wherein.

L~invention décrit un procédé pour préparer des benzothiazinoindoles substitués répondant à la formule générale (I) où R1, R2, et R4 sont indépendamment choisis parmi un atome d~hydrogène, un groupe chloro, fluoro, amino, nitro, cyano, CHO, alkyle en C1-C3, perhalogéno(alkyle en C1-C3), alcoxy en C1-C3, aryle, aralkyle, aralcoxy, hétérocyclique en C5-C7, hétérocycloalkyle en C5-C7, hétérocyclyloxy en C5-C7, acyle, acétyle, alkylamino, aminoalkyle, amide, hydroxyalkyle, acide carboxylique et ses dérivés, tandis que R3 est choisi parmi un atome d~hydrogène, un groupe alkyle en C1-C3, aryle et acide carboxylique et ses dérivés, ledit procédé comprenant la cyclisation du composé répondant à la formule générale II, (à savoir, un 1-benzènesulfonyl-7-bromo-1H-indole substitué), la formule (II) où R1, R2, R3 et R4 utilisant un catalyseur et des solvants appropriés dans celui-ci.

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