| 摘要 |
1,199,630. Phenylethanolamine derivatives. DRACO, LUNDS FARMACEVTISKA A.B. 18 Oct., 1967 [19 Oct., 1966], No. 47505/67. Heading C2C. Compounds of the general formula (R = tert.-butyl, cyclobutyl, cyclopentyl; R<SP>5</SP> = OH, C 1-5 alkanoyloxy) and their salts are prepared by (a) reducing a compound of the formula (R<SP>3</SP> = H or group replaceable by H) in the presence of RNH 2 , followed by replacement of R<SP>3</SP> if necessary; (b) reacting a compound of the formula with RR<SP>4</SP>NH (R<SP>4</SP>=H, aralkyl), followed by replacement of R<SP>3</SP>'<SP>4</SP>, if necessary; (c) reducing a compound of the formula followed by replacement of R<SP>3</SP>'<SP>4</SP> if necessary; or (d) hydrogenating a compound of the formula reacting the product with cyclobutanone or cyclopentanone, further hydrogenating the reaction mixture and replacing R<SP>3</SP> if necessary; optionally followed in each case by salt formation. The preparation of starting materials for processes (a), (b), (c) and (d) by standard methods and of ethyl 3,5-dihydroxybenzoate, 3,5- dibenzyloxybenzoic acid, 3,5-dibenzyloxybenzoyl chloride, 3,5 - dibenzyloxy - # - bromoacetophenone, 3,5 - dibenzyloxy - # - chloroacetophenone and 3,5-dibenzyloxyacetophenone is described. The compounds of the invention are bronchodilators, and may be administered in the form of pharmaceutical preparations containing them in association with a carrier. |
