A process for the preparation of carvedilol of formula (I) (I) either in
enantiomeric substantially pure form, or as an enantiomeric mixture,
optionally as a pharmaceutically acceptable salt thereof, which process
comprises reacting 2,3-eopxypropoxy carbazole of formula (II) (II) or the
R or S enantiomer thereof, with
N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) (V) to yield
benzyl carvedilol of formula (VI) (VI) which is debenzylated by catalytic
hydrogenation to yield carvedilol of formula (I), either in enantiomeric
substantially pure form, or as an enantiomeric mixture, and if desired
reacting the thus formed carvedilol of formula (I) with an inorganic or
organic acid to yield a pharmaceutically acceptable salt thereof, and/or,
if desired, separating the enantiomers. The above process is
characterised in that reaction of said 2,3-epoxypropoxy carbazole of
formula (II) with said N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of
formula (V) is carried out in water as the reaction medium. The present
invention further provides carvedilol of formula (I) prepared by a
process as described above, and pharmaceutical compositions containing
the same and therapeutic uses thereof. ##STR00001##