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Title:
METHOD FOR SYNTHESIZING DEGARELIX ACETATE
Document Type and Number:
WIPO Patent Application WO/2021/026800
Kind Code:
A1
Abstract:
Disclosed is a method for synthesizing Degarelix acetate. The method comprises: S1, carrying out a condensation reaction with the first six amino acids of Degarelix in sequence by using a Rink Amide MBHA resin as a carrier so as to obtain a hexapeptide resin fragment III; S2, carrying out a condensation reaction with the last four amino acids of Degarelix in sequence by using a CTC resin as a carrier so as to obtain a tetrapeptide resin fragment I; S3, cutting the tetrapeptide resin fragment I to obtain a tetrapeptide fragment II; S4, carrying out a condensation reaction on the hexapeptide resin fragment III and the tetrapeptide fragment II under the action of MYMsA and/or MYTsA so as to obtain a whole-peptide resin; S5, cutting the whole-peptide resin to obtain Degarelix; and S6, carrying out acetic acid salt conversion on the Degarelix to obtain Degarelix acetate.

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Inventors:
LI JIUYUAN (CN)
LI CHANGFENG (CN)
LI BANGHONG (CN)
ZHU ZILI (CN)
LI XINYONG (CN)
Application Number:
PCT/CN2019/100530
Publication Date:
February 18, 2021
Filing Date:
August 14, 2019
Export Citation:
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Assignee:
ASYMCHEM LIFE SCIENCE TIANJIN CO LTD (CN)
International Classes:
C07K7/23; C07K1/04; C07K1/06; C07K1/34
Foreign References:
CN103351428A2013-10-16
CN107022002A2017-08-08
CN106589071A2017-04-26
CN103992378A2014-08-20
Other References:
HUANG YU, CHEN JINGSHUN, LIU BAOMIN, WANG HUA, ZHANG LU, CHEN ZHENGBANG, ZHANG YINSHENG: "An efficient synthesis of deuterium-labeled degarelix acetate, a third-generation gonadotropin-releasing hormone receptor antagonist", JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, JOHN WILEY & SONS LTD., GB, vol. 61, no. 4, 1 April 2018 (2018-04-01), GB, pages 355 - 361, XP055781965, ISSN: 0362-4803, DOI: 10.1002/jlcr.3567
Attorney, Agent or Firm:
KANGXIN PARTNERS, P.C. (CN)
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