Title:
METHOD FOR FULLY LIQUID-PHASE SYNTHESIS OF GRNH NONAPEPTIDE AMIDE ANALOG
Document Type and Number:
WIPO Patent Application WO/2023/030277
Kind Code:
A1
Abstract:
Provided is a method for fully liquid-phase synthesis of a GRnH nonapeptide amide analog, which belongs to the technical field of medicine synthesis. The method comprises respectively synthesizing a "Trp-Ser-Tyr" fragment, an "R-Leu" fragment, a "Pyr-His" fragment and "Arg-Pro-Hunan T", wherein, R = D-Ala (alarelin), D-Leu (leuprorelin), D-Trp (deslorelin) and D-His (histrelin), and obtaining the GRnH nonapeptide amide analog with high yield and high purity by means of a "3 +2 +2 +2" fragment condensation method. The synthesis method is environmentally friendly, mild, and free of any highly toxic and poisonable reagents. The cost is greatly reduced and the synthesis method is very suitable for large-scale production.
Inventors:
SUN PENGCHENG (CN)
PAN JING (CN)
WU JUNYONG (CN)
TANG YONGBO (CN)
DU YIXIONG (CN)
GUO LIN (CN)
PAN JING (CN)
WU JUNYONG (CN)
TANG YONGBO (CN)
DU YIXIONG (CN)
GUO LIN (CN)
Application Number:
PCT/CN2022/115636
Publication Date:
March 09, 2023
Filing Date:
August 29, 2022
Export Citation:
Assignee:
HUNAN MICRO PEPTIDE BIOMEDICAL CO LTD (CN)
International Classes:
C07K7/23; C07K1/02; C07K1/06; C07K1/08; C07K1/30
Domestic Patent References:
| WO1997034923A1 | 1997-09-25 | |||
| WO2020057088A1 | 2020-03-26 |
Foreign References:
| CN112279894A | 2021-01-29 | |||
| CN109438560A | 2019-03-08 | |||
| US20150166602A1 | 2015-06-18 |
Other References:
SONG, YUN; ZHONG, XIA; CHEN, NIAN-GEN: "Synthesis of Buserelin Using Solid-liquid Combination Method", GUANGZHOU CHEMICAL INDUSTRY, vol. 48, no. 5, 31 March 2020 (2020-03-31), pages 46 - 48, 110, XP009544214, ISSN: 1001-9677
MOHR M.A.; WONG A.M.; TOMM R.J.; SOMA K.K.; MICEVYCH P.E.: "Pubertal development of estradiol-induced hypothalamic progesterone synthesis", HORMONES AND BEHAVIOR, ACADEMIC PRESS, NEW YORK, NY, US, vol. 111, 1 January 1900 (1900-01-01), US , pages 110 - 113, XP085690393, ISSN: 0018-506X, DOI: 10.1016/j.yhbeh.2018.12.007
MOHR M.A.; WONG A.M.; TOMM R.J.; SOMA K.K.; MICEVYCH P.E.: "Pubertal development of estradiol-induced hypothalamic progesterone synthesis", HORMONES AND BEHAVIOR, ACADEMIC PRESS, NEW YORK, NY, US, vol. 111, 1 January 1900 (1900-01-01), US , pages 110 - 113, XP085690393, ISSN: 0018-506X, DOI: 10.1016/j.yhbeh.2018.12.007
Attorney, Agent or Firm:
BEIJING WEISHENGDA INTELLECTUAL PROPERTY AGENCY (GENERAL PARTNERSHIP) (CN)
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