Synthesis of aryloxypropanolamines and arylethanolamines

Details Synthesis of aryloxypropanolamines and arylethanolamines Synthesis of aryloxypropanolamines and arylethanolamines

C - Chemistry, Metallurgy

07

C

260/602, 260/369

C07C 217/72 (2006.01) C07C 41/22 (2006.01) C07C 229/34 (2006.01) C07D 285/10 (2006.01) C07D 303/22 (2006.01) C07D 405/12 (2006.01)

Patent

CA 1282787

ABSTRACT OF THE DISCLOSURE Described is a process for preparing a racemic or chiral aryloxypro- panolamine (1) or arylethanolamine (2) of the formula Image 1 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, alkoxy- alkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R3 and R5 are not hydrogen when B is -NR7SO2R3 or -NR2COOR5, or R3 and R4 may together with N form a 5- to 7-membered hetero- cyclic group. The process can be used to prepare beta-blocking agents, useful in the treatment of cardiac conditions.

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