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Practical synthesis of a peptidomimetic thrombin inhibitor
Authors:Serge Wilmouth  Christel Bufferne-Perret  Christine Flouzat  Grégoire Humblot  Christiane Ray  Nadine Simbille
Institution:Schering-Plough France, Preclinical Development Center, 20 rue Henri Goudier, B.P. 140, 63203 Riom Cedex, France
Abstract:Compound 1 is a low molecular weight thrombin inhibitor developed for treatment of deep vein thrombosis and cardiovascular diseases. We herein report our efforts to develop a robust, efficient and reproducible process suitable for large-scale synthesis of compound 1.
Keywords:Low molecular weight thrombin inhibitor  Peptidomimetic  α-Hydroxy amide oxidation  Impurity identification  Process development and scale-up
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