The present invention relates to a process for the preparation of
acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides of the
formula I, ##STR00001## in which the anions X are physiologically
acceptable anions, and their analogs, which are effective inhibitors of
the blood coagulation factor Xa and which can be used, for example, for
preventing thromboses. The process according to the invention comprises
the coupling of
2-[2-acetylamino-3-(4-amidinophenyl)propionylamino]-2-cyclohexylacetic
acid, which is obtained from
2-[2-acetylamino-3-(4-cyanophenyl)acryloylamino]-2-cyclohexylacetic acid
by asymmetric hydrogenation and conversion of the cyano group into the
amidine, or a salt thereof, with a
3-(2-amino-2-carbamoylethyl)-1-methylpyridinium salt or a salt thereof.
The invention furthermore provides starting materials and intermediates
for this process, processes for their preparation and
acetyl-(S)-4-amidiniophenylalanyl-(S)-cyclohexylglycyl-(S)-(1-methyl-3-py-
ridinio)alaninamide as ditosylate salt.