<p>Disclosed is a three step process for the manufacture of pseudo proline dipeptides of the formula (I) wherein R<SUP>1</SUP> is a side chain of an alpha amino acid , R<SUP>2</SUP> is an amino protecting group and R<SUP>3</SUP> and R<SUP>4</SUP> are independently selected from hydrogen or C<SUB>1-4</SUB>-alkyl, R<SUP>5</SUP> is hydrogen or methyl starting from an amino acid derivative of the formula (II) wherein R<SUP>1</SUP> and R<SUP>2</SUP> are as above. Pseudo proline dipeptides can be used as reversible protecting groups for Ser, Thr and Cys and thus are versatile tools in peptide chemistry.</p>
申请公布号
WO2008000641(A1)
申请公布日期
2008.01.03
申请号
WO2007EP55988
申请日期
2007.06.18
申请人
F. HOFFMANN-LA ROCHE AG;AMMANN, THOMAS;GOETZOE, STEPHAN;THERN, BERND;WELZ, SANDRA;WOLTER, KLAUS-JUERGEN