| abstract |
The present invention relates to a process for the preparation of acetyl-amidiniophenylalanylcyclohexylglycyl-pyridinioalanilamide of formula (I), wherein the anions are X-physiologically acceptable anions, and their analogs, which are effective inhibitors of blood coagulation factor Xa, and which can be used, for example, for the prevention of thrombosis . The process according to the present invention consists of coupling 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 to amidine, or a salt thereof, with 3- (2-amino-2-carbamoylethyl) 1-methylpyridinium salt, or a salt thereof. The present invention further provides starting materials and intermediates for this process, processes for their preparation and (S) -4-amidinophenylalanyl- (S) -cyclohexylglycyl- (S) - (1-methyl-3-pyridinio) alaninamide, as a ditosylate salt. |