abstract |
The present invention relates to a process for the preparation of peptides of the formula (X), wherein A is a natural or unnatural amino acid, an azaamino acid or an imino acid, and an integer of 1 to 50, preferably 1 to 30. and A azaamino acid, as well as physiologically acceptable salts thereof, by solid phase synthesis, wherein the spacer is converted to an acylation form, which is then reacted with a suitable formic acid derivative and the corresponding amino acid hydrazide, optionally converting the protecting group to a basic or weak acid labile protecting group, the spacer thus obtained bound to the resin, sequentially constructing the desired peptide, then cleaving the peptide from the resin and optionally converting it to a physiologically acceptable salt. |