| 摘要 |
The present invention provides for an efficient process of making Bivalirudin in solution that is high in yield, scalable for commercial production, and of high purity compared to the solid-phase peptide synthesis method. The process comprises the stepwise synthesis of amino acid segments S1 (Boc-D-PheProArg(HCI)ProOH), S2 (FmocGlyGlyGlyGlyAsnGlyOH), S3 (AspPheGlu(tBu)Glu(tBu)lIeProOBn), S4 (Glu(tBu)Glu(tBu)Tyr(tBu)LeuOtBu), and the coupling together of these segments to produce Bivalirudin. |
