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Paper | Special issue | Vol 74, No. 1, 2007, pp.437-445
Published online, 5th October, 2007
DOI: 10.3987/COM-07-S(W)22
Practical and Efficient Processes for the Preparation of 4-(4-Aminophenyl)morpholin-3-ones on a Larger Scale: Precursor of Factor Xa Inhibitors

Werner W. K. R. Mederski,* Peter Ludwig Wendel, and Markus Woissyk

*Preclinical Pharmaceutical Research, Merck KGA, Frankfurter Str. 250, 64271 Darmstadt, Germany

Abstract

Factor Xa inhibitors are interesting targets for the development of antithrombotic agents. Our personal efforts in the discovery of small molecule inhibitors led to the compounds EMD 495235 and EMD 503982, which entered preclinical and clinical studies, respectively. Therefore, kilograms of both drugs in particular 4-(4-aminophenyl)morpholin-3-one moieties have to be provided. The scale-up results of these special P-4 ligands will be described herein.