Aplha-substituted-3-benzyl-benzofurans

Claim 1

A compound of the formula ##STR33## wherein R 1 is OH, OCO (C 1 -C 6 alkyl), OCO (aryl), OSO 2 (C 4 -C 6 alkyl), OCOO (C 1 -C 6 alkyl), OCOO (aryl), OCONH (C 1 -C 6 alkyl), or OCON (C 1 -C 6 alkyl) 2 ; R 2 is aryl, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, or 4-cyclohexanol; R 3 is O (CH 2 ) 2 or O (CH 2 ) 3 ; R 4 and R 5 are optionally CO (CH 2 ) 2 CH 3 , CO (CH 2 ) 3 CH 3 , C 1 -C 6 alkyl, or R 4 and R 5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrrolidine, 3-methylpyrrolidine, 3,3-dimethylpyrrolidine, 3,4-dimethylpyrollidine, azepine, or pipecoline; R 6 is ##STR34## wherein each of R 7 and R 8 is taken separately and represents H, C 1 -C 6 -alkyl, 2-hydroxyethyl, or 2-fluoroethyl, with the proviso that (1) R 7 and R 8 are not both H; (2) R 7 and R 8 are not both C 1 -C 6 -alkyl; and (3) when either R 7 or R 8 is H, then the other is not C 1 -C 6 -alkyl; or both R 7 and R 8 are taken together with the nitrogen and form a ring which is pyrrolidine, piperidine, azepine, or morpholine and which may optionally be substituted by one or two methyl groups, or ##STR35## wherein each of R 10 and R 11 is taken separately and represents H or C 1 -C 2 , or both R 10 and R 11 are taken together with the nitrogen and represent a ring which is a pyrrolidine, piperidine, azepine or morpholine and which may optionally be substituted by one or two methyl groups, and R 12 is hydrogen, methyl, or ethyl; and pharmaceutically acceptable salts thereof.