Aplha-substituted-3-benzyl-benzofurans

A compound of the formula ##STR33## wherein R.sub.1 is OH, OCO (C.sub.1 -C.sub.6 alkyl), OCO (aryl), OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), OCOO (C.sub.1 -C.sub.6 alkyl), OCOO (aryl), OCONH (C.sub.1 -C.sub.6 alkyl), or OCON (C.sub.1 -C.sub.6 alkyl).sub.2 ;

• R.sub.2 is aryl, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, or 4-cyclohexanol;
• R.sub.3 is O (CH.sub.2).sub.2 or O (CH.sub.2).sub.3 ;
• R.sub.4 and R.sub.5 are optionally CO (CH.sub.2).sub.2 CH.sub.3, CO (CH.sub.2).sub.3 CH.sub.3, C.sub.1 -C.sub.6 alkyl, or R.sub.4 and R.sub.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.sub.6 is ##STR34## wherein each of R.sub.7 and R.sub.8 is taken separately and represents H, C.sub.1 -C.sub.6 -alkyl, 2-hydroxyethyl, or 2-fluoroethyl, with the proviso that (1) R.sub.7 and R.sub.8 are not both H;
• (2) R.sub.7 and R.sub.8 are not both C.sub.1 -C.sub.6 -alkyl;
• and
• (3) when either R.sub.7 or R.sub.8 is H, then the other is not C.sub.1 -C.sub.6 -alkyl;
• or both R.sub.7 and R.sub.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.sub.10 and R.sub.11 is taken separately and represents H or C.sub.1 -C.sub.2, or both R.sub.10 and R.sub.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.sub.12 is hydrogen, methyl, or ethyl;
• and pharmaceutically acceptable salts thereof.