| 摘要 |
Alkanolamines - (I) where Y = O - R1, R3, R4 = H - (R2 = Et - (B = 4-Cl-3-Me-phenyl; 3,5-Me2-phenyl - (R2 = n-Pr - (B = 3-tolyl; 3,5-Me2-phenyl; 2,5-Cl2-phenyl; 3-MeO-phenyl - or Y = O R1 = H, opt. substd. alkyl, alkenyl, aralkyl - R3, R4 = H, alkyl - R2 = branched alkyl, substd. alkyl, cycloalkyl alkenyl, opt. substd. ( >7C) aralkyl - B = phenyl substd. at 3 or 4 only, or is substd. at 2 only by: iodine, HO, NO2, acyl, aryl, aryloxy, alkylaryloxy, arylthio, arylsulphonyl, arylamino, aralkyl, aralkoxy; or it is substd. by up to 5 substituents, - or Y = S R1 = H R3, R4 = H, alkyl - R2 = H, alkyl, cycloalkyl, alkenyl, aralkyl - B = substd. phenyl - together with their esters and salts, but excluding the following 1-(substd. phenoxy)-3-(substd. amino)-2-propanols:- - 1- 4-Cl3- 1-Me-2-Ph-ethyl; cyclohexyl; - isoamyl - 2,6-Me2 isopropyl - 4-t-amylisobutyl; isoamyl; isopropyl - 4-t-butyl isoamyl - 2-MeO isobutyl; N-isopropyl-N-Me. - beta-Adrenergic blockers, useful in the treatment of coronary arterial disease. - A mixt. of 1-Cl-3-(2,3-Me2-phenoxy)-2-propanol (II) (2.03 pts.) and isopropylamine (15 pts.) is heated at 70-80 deg. for 10 hrs - Working up gives 1-(2,3-Me2-phenoxy)-3-isopropylamino-2-propanol, m.p. 110-2 deg. (petrol).
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