| 摘要 |
<p>1,214,012. Phenylethanolamine derivatives. ALLEN & HANBURYS Ltd. 13 Dec., 1968 [21 Dec., 1967], No. 58012/67. Heading C2C. Compounds of the general formula (I) (R 1,4 = H, C 1-6 alkyl; R 2 = H, R 3 CO-(R 3 = H, C 1-6 alkyl optionally substituted by one or more halogen atoms or hydroxyl, amino or amido groups, aryl, aralkyl, OR 1 ), -CONR 1 R 3 , R 3 SO 2 (R 3 ŒH, OR 1 ); R 5,6 = H, C 1-6 alkyl optionally substituted by an amino, alkylated amino or heterocyclic group, aralkyl, substituted aralkyl, aroxyalkyl, substituted aroxyalkyl, cycloalkyl) and their acid addition salts are prepared by (a) acylating a compound of the formula (II) (R 2 = H; R 5,6 Œ H) and hydrogenolysing the product, (b) reducing a compound of the formula (III) (c) condensing a compound of the formula (II) (R 1,2 = H) with an aldehyde or ketone and reducing the product, or (d) condensing a compound of the formula (IV) (R 7 = protecting group) with R 1 NH 2 , acylating the product if necessary, converting the resulting compound of the formula (VI) to the corresponding haloketone, reacting the latter with R 5 R 6 NH, reducing the CO group to CHOH and removing R 7 by hydrolysis or hydrogenolysis, optionally followed in each case by salt formation. The above compounds possess stimulant or blocking actions on adrenergic receptors, and may be administered in the form of pharmaceutical or veterinary preparations containing them together with a carrier.</p> |
