| 摘要 |
<p>1474775 Isoquinolines SANDOZ Ltd 3 Oct 1974 [8 Oct 1973] 42909/74 Heading C2C Compounds of the general formula I (R=C 3-7 alkyl or cycloalkyl, C 3-7 cycloalkyl substituted by C 1-4 alkyl, C 5-9α-dialkylpropynyl orα-dialkylallyl, C 2-7 hydroxyalkyl in which the OH group is separated from the nitrogen atom by at least two carbon atoms, phenethyl optionally substituted by halogen or C 1-4 alkyl or alkoxy, adamantyl; R 1 =H, halogen, C 1-4 alkyl or alkoxy, 5, 6 or 7-CF 3 , 4 or 5-NO 2 or C 1-4 alkanoylamino; R 2 =H or (R 1 = C 1-4 alkyl) C 1-4 alkyl or (R 1 = C 1-4 alkoxy) C 1-4 alkoxy; provided that the 8-position of the isoquinoline ring is unsubstituted and no 3 or 4-F substituent is present) and their salts are prepared by (a) reacting a compound of the Formula II (X = leaving atom or group) with or (b) hydrolysing a compound of the Formula IV (ZZ<SP>1</SP>C = hydrolysable group), optionally followed by salt formation. The 2,3-dihydroxypropylamines are prepared by reacting 2,3-dihydroxypropyl chloride or glycidol with RNH 2 , the compounds of Formula IV are prepared by reacting a compound of Formula II with a compound of Formula VI and the latter compounds are prepared by reacting the appropriate 2,3-dihydroxypropylamine and aldehyde or ketone. 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> |
