Synthesis of peptides labeled selectively on amino groups, useful in biotechnology and diagnosis, uses selectively removable protecting group at labeling position

摘要

Method for selectively labeling amino groups in peptides (I), prepared by chemical solid-phase synthesis. Method for selectively labeling amino groups in peptides (I), prepared by chemical solid-phase synthesis comprises (1) incorporating, during synthesis and at the positions intended for labeling, an amino acid synthon in which amino is protected by a group (PG1) that is functionally different from the group (PG2) on amino groups that are not intended for labeling; (2) at the end of synthesis, selective removal of PG1 and release of (I) from its carrier; (3) reacting the released peptide, in solution, with a labeling reagent, specifically at free amino; and (4) removal of PG2 and conventional purification of the product.