Peptide compound and a process for the preparation thereof
The present invention concerns glycoprotein IIa/IIIb antagonists and platelet aggregation inhibitors of the formula (I): STR1 wherein R1 is aryl which may have one or more suitable substituent(s), R2 is carboxy(lower)alkyl or protect
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(2008/06/13)
Efficient Kg-Scale Synthesis of Thrombin Inhibitor CRC 220
Potent thrombin inhibitor 2 is prepared in 10 steps with 20percent overall yield from commercial 4 on a kg-scale by the convergent approach depicted in Schemes 1 and 2.The (R)-configuration of the 4-amidinophenylalanine piperidide moiety is controlled by asymmetric hydrogenation.A novel method, the hydrogenolysis of amidoximes 11 and 21, is employed to attain a particularly clean transformation of the cyano into the amidinium functionality.Despite of the amorphous nature of target compound 2, the approach is devoid of any chromatographic purification.