PROCESS FOR THE MANUFACTURE OF DEGARELIX AND ITS INTERMEDIATES
申请人:Kalita Dipak
公开号:US20130281662A1
公开(公告)日:2013-10-24
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 ε-amino protecting group Pε from a Degareiix precursor according to formula P
4
)(Pε)Ac-AA
1
-AA
10
-NH
2
in an organic solvent comprising the precursor and a cleaving agent dissolved therein: wherein P
4
is a hydroxyl-protecting group or hydrogen, preferably hydrogen.
The present invention provides a method of preparing an intermediate for LHRH antagonists, which requires fewer steps than conventional methods and provides the intermediate in high yield and high purity.