2,1-benzisothiazoles and preparation thereof

Details 2,1-benzisothiazoles and preparation thereof 2,1-benzisothiazoles and preparation thereof

C - Chemistry, Metallurgy

07

D

260/309.1, 260/2

C07D 275/04 (2006.01) C07D 417/04 (2006.01)

Patent

CA 1107730

-1- ABSTRACT OF THE DISCLOSURE Novel 3-(Substituted-amino-2,1-benziso- thiazoles useful as anti-inflammatory agents having the Formula Image I wherein R1 is hydrogen, metheyl or ethyl; R2 is IA Image , Image or -Y-NR4R5; or R1 and R2 taken together with the nitro- gen atom are piperazinyl, N-lower alkylpiperazinyl or N-phenylpipazinyl; R3 is methyl or ethyl; R4 and R5 are hydrogne, lower-alkyl or hydroxy-lower alkyl; or R4 and R5 taken togther with the nitrogen atom are pyrrolidino, piperidino, hexamethyleneimino, piperzinyl, N-lower alkylpiperazinyl or N-phenyl- piperazinyl; Y is an alkylene group containing from 2 to 8 carbon atoms and separating the two nitrogen atoms by at least 2 carbon atoms; X occupies any of positions 4,5,6, or 7 and is selected from the group consisting of methoxy and halo; and n is 1 or 2; or 0, 1 or 2 when R2 is (IA), said compounds are prepared by reductive cyclization of appropriately substituted 2-nitro- thiobenzamides or by reaction of 3-chloro-2,1-benz- isothiazoles with suitably substituted amines.

308890

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