SYNTHESIS OF ARYLOXYPROPANOLAMINES AND ARYLETHANOLAMINES

摘要

A process for preparing a racemic or chiral aryloxypropanolamine (1) or arylethanolamine (2) of the formula (1) or (2) wherein Ar is aryl, substituted aryl, heteroaryl, or aralkyl and R is alkyl, substituted alkyl, aralkyl or WB wherein W is a straight or branched chain alkylene of from 1 to about 6 carbon atoms and wherein B is -NR2COR3, -NR2CONR3R4, -NR2SO2R3, -NR2SO2NR3R4, or -NR2COOR5, where R2, R3, R4, and R5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynil, aryl, heteroaryl, or aralkyl, except that R3 and R5 are not hydrogen when B is -NR2SO2R3 or -NR2COOR5, or R3 and R4 may together with N form a 5- to 7-membered heterocyclic group. The process can be used to prepare beta-blocking agents, useful in the treatment of cardiac conditions.