Desmopressin synthetic analogs protected in C-terminal sequence against carboxyamidase cleavage

摘要

C-terminal sequence and fission carboxyamidase general formula I in a kind of synthetic analogues Desmopressine protection; wherein A is [D-Arg] GlyNHR (substance 1) or [D-Arg] NHR (substance 2), and wherein R is alkyl, contains 1 to 4 carbon atom. Its preparation is the functional group for making the related Desmopressine of the amino acid sequence N-protected of hydroxybenzotriazole ester act on the connections of NHR-CH2 containing general formula, and wherein R is alkyl, contains 1 to 4, usual 2 carbon atoms. In the peptide that completion entirely needs, the peptide and resin are dry, protecting group, and mixed fluoride hydrogen and methyl phenyl ethers anisole, from resin, peptide is dissolved in spirit of vinegar, and freeze-drying and cyclisation are to undertake disulphide bridges by closure, and then its isolation passes through efficient liquid chromatography.IMAGE