Chemoenzymatic synthesis of the enantiomerically pure 1,2,3,4-tetrahydroquinoline moiety of the antithrombotic (21R)- and (21S)-argatroban |
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Authors: | Patrizia Ferraboschi Samuele Ciceri Paride Grisenti |
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Institution: | 1. Dipartimento di Biotecnologie Mediche e Medicina Traslazionale, Università Statale di Milano, Via Saldini 50, 20133 Milano, Italy;2. EUTICALS SpA, Via Volturno 41/43, 20089 Rozzano (Mi), Italy |
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Abstract: | The synthetic antithrombotic argatroban is a dipeptide between the nonproteogenic (2R,4R)-4-methyl-2-piperidine carboxylic acid and l-arginine, in turn bonded to a 3-methyltetrahydroquinoline sulfonyl group; the drug is usually prepared and administered as a mixture of C-21-diastereoisomers. By means of a biocatalytic transformation enantiomerically pure (R)- and (S)-synthons, suitable for the synthesis of separate (21R)- and (21S)- argatroban, were obtained. |
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