| 摘要 |
<p>1298017 Propanolamines HASSLE AB 20 May 1970 [21 May 1969] 24499/70 Heading C2C Compounds of the general formula (R<SP>1</SP> = isopropyl, tert-butyl; R<SP>2</SP> = CH 2 CH 2 OCH 3 , and their salts are prepared by (a) reacting a compound of the formula (X = oxiranyl, 2-halo-1-hydroxyethyl) with R<SP>1</SP>NHCONHR<SP>1</SP> or R<SP>1</SP>NH 2 , (b) reacting the corresponding primary amine with acetone under reducing conditions or with an appropriate alkyl halide, (c) hydrolysing a compound of the formula (R<SP>3</SP> = hydrolysable group) or (d) hydrolysing or pyrolysing a compound of the formula (R<SP>4</SP>'<SP>5</SP> = H, alkyl, aralkyl, aryl), (e) hydrolysing or hydrogenolysing a compound of the formula (R<SP>6</SP> = protecting group), (f) reacting a compound of the formula (M = cation) with R<SP>1</SP>NHCH 2 X, (g) reducing a compound of the formula (A = CH(OH)CO, COCH 2 ), (h) hydrolysing a compound of the formula (R<SP>7</SP> = alkyl, aralkyl, aryl) or (i) hydrogenating a compound of the formula (R<SP>8-11</SP> = H or halogen provided that at least one is halogen), optionally followed in each case by resolution and/or salt formation. The preparation of starting materials for process (a) in which X = oxiranyl and the parent phenols R<SP>2</SP>OC 6 H 4 OH by standard methods is described. The above compounds are #-adrenergic blocking agents, and may be administered in the form of pharmaceutical preparations containing them in association with a carrier.</p> |
