PROCESS FOR THE MANUFACTURE OF DEGARELIX AND ITS INTERMEDIATES

摘要

The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degareiix, its amino-protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degareiix itself. The manufacturing process comprises the step of cleaving the &egr;-amino protecting group P&egr; from a Degareiix precursor according to formula {P4)(P&egr;)Ac-AA1-AA10-NH2 in an organic solvent comprising the precursor and a cleaving agent dissolved therein: wherein P4 is a hydroxyl-protecting group or hydrogen, preferably hydrogen.