A short synthesis of argatroban. a potent selective thrombin inhibitor. |
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Authors: | J Cossy D Belotti |
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Affiliation: | Laboratoire de Chimie Organique associé au CNRS, ESPCI, 10 rue Vauquelin, 75231 Cedex 05, Paris, France. janine.cosy@espci.fr |
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Abstract: | Argatroban was synthesized in seven steps from 4-methylpiperidine. The condensation of (+/-)-trans-benzyl 4-methylpipecolic acid ester with N(alpha)-Boc-N(omega)-nitro-L-arginine led to two diastereomers that were separated. One of them is the precursor of argatroban. |
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