| 摘要 |
A method for producing bivalirudin using solid phase peptide synthesis by: a) condensing Fmoc-Asn(Trt)-Gly-OH with a peptide resin of Asp(OtBu)11-Phe12-Glu(OtBu)13-Glu(OtBu)14-Ile15-Pro16-Glu(OtBu)17-Glu(OtBu)18-Tyr(tBu)19-Leu20-Resin; b) removing Fmoc-; c) condensing Fmoc-Gly-Gly-Gly-Gly-OH with the peptide resin; d) separately condensing Pro, Arg, Pro, and Phe with the peptide resin from C-terminal to N-terminal to yield a peptide resin of Boc-D-Phe1-Pro2-Arg(Pbf)3-Pro4-Gly5-Gly6-Gly7-Gly8-Asn(Trt)9-Gly10-Asp(OtBu)11-Phe12-Glu(OtBu)13-Glu(OtBu)14-Ile15-Pro16-Glu(OtBu)17-Glu(OtBu)18-Tyr(tBu)19-Leu20-Resin; and e) in the presence of a cleavage agent, separating a peptide from the peptide resin to yield bivalirudin represented by Formula VI. The method is low in cost and the resultant bivalirudin has high purity.
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