Process for the manufacture of Degarelix and its intermediates
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United States of America Patent
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Feb 16, 2016
Grant Date -
Oct 24, 2013
app pub date -
Oct 26, 2011
filing date -
Oct 27, 2010
priority date (Note) -
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Abstract
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 {P4)(Pε)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.
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