2,3,4,5-tetrahydro-1-benzoxepin-3,5-dione derivatives

Details 2,3,4,5-tetrahydro-1-benzoxepin-3,5-dione derivatives 2,3,4,5-tetrahydro-1-benzoxepin-3,5-dione derivatives

C - Chemistry, Metallurgy

07

D

260/355.5

C07D 313/08 (2006.01)

Patent

CA 1159840

ABSTRACT OF THE DISCLOSURE The present invention provides 2,3,4,5-tetrahydro-1- benzoxepin-3,5-dione derivatives of the following Formula II Image II wherein R3 and R4 independently of one another are halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkylthio or one of R3 and R4 are halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkylthio, trifluoro- methyl or nitro and the other is hydrogen, with the proviso that R3 is not bromine when R4 is methyl, which are intermediates in the preparation of 3-amino-1-benzoxepin-5(2H)-one derivatives corresponding to the Formula I: Image I wherein: R1 and R2 independently of one another are hydrogen, C1-C5 alkyl, C1-C5 alkyl substituted with a terminal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4-ethylenedioxy group, C2-C5 alkyl, C2-C5 alkyl substituted with terminal hydroxy or methoxy or C3- C4 alkenyl; or one of R1 and R2 are hydrogen or a C1-C5 alkyl and the other is a C2-C5 alkyl substituted with a terminal NR5R6; R5 and R6 independently of one another are hydrogen or C1-C5 alkyl; or R5 and R6 are together a 5 to 7 member ring, or R5 and R6 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or nitrogen; R1 and R2 are together a 5 to 7 member ring, or R1 and R2 are together a 5 to 7 member ring having heterogeneous oxy- gen, sulfur or NR7; R7 is hydrogen, methyl, benzyl or phenyl; and R3 and R4 are as above; and pharmaceutically acceptable acid addi- tion salts thereof, which are useful in the treatment of spasms of the stomach-intestinal tract.

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