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elagolix

elagolix Structure
CAS No.
834153-87-6
Chemical Name:
elagolix
Synonyms
Elagoli;NBI 56418;(R)-4-((2-(5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)-1-phenylethyl)amino)butanoic acid;CS-2232;CS-2011;ABT-620;elagolix;Elagolix-d6;(R)-Elagolix;Elagolix CAS
CBNumber:
CB51518509
Molecular Formula:
C32H30F5N3O5
Molecular Weight:
631.59
MOL File:
834153-87-6.mol
MSDS File:
SDS
Modify Date:
2024/7/2 8:55:10
Request For Quotation

elagolix Properties

Boiling point 728.6±70.0 °C(Predicted)
Density 1.350
storage temp. Store at -20°C
solubility DMSO : ≥ 100 mg/mL (158.33 mM)
pka 4.40±0.10(Predicted)
form Solid
color White to off-white
InChIKey HEAUOKZIVMZVQL-VWLOTQADSA-N
SMILES C(O)(=O)CCCN[C@H](C1=CC=CC=C1)CN1C(=O)N(CC2=C(C(F)(F)F)C=CC=C2F)C(C)=C(C2=CC=CC(OC)=C2F)C1=O

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS08
Signal word  Danger
Hazard statements  H360
Precautionary statements  P201-P202-P280-P308+P313-P405-P501

elagolix Chemical Properties,Uses,Production

Description

Elagolix is a gonadotropin-releasing hormone(GnRH) receptor antagonist indicated for the management of moderate to severe pain associated with endometriosis. Elagolix is an orally administered,nonpeptide small molecule gonadotropin-releasing hormone(GnRH) receptor antagonist that inhibits endogenousGnRH signaling by binding competitively to GnRH receptors in the pituitary gland.
Elagolix results in dose-dependent suppression of luteinizing hormone(LH) and follicle-stimulating hormone(FSH) leading to decreased blood leveis of the ovarian sex hormones, estradiol and progesterone.Elagolix causes a dose-dependent decrease in bone mineral density (BMD).BMD loss is greater with increasing duration of use and may not be completely reversible after stopping treatment.
As milk production is dependent on at least minimal levels of estrogen, this product may reduce milk production.

Uses

Elagolix has a potential role for treating uterine bleeding associated to uterine myomas. Elagolix is also used in the methods for treatment of estrogen-dependent disorders including gonadotropin-releasing hormone (GnRH) antagonists in combination with add-back therapy.

Preparation

Elagolix was a gonadotropin-releasing hormone antagonist. It was approved in 2018 by FDA via priority review for clinical treatment of endometriosis. Based on retrosynthetic analysis, five reported synthesis routes of elagolix were summarized. They were compared and evaluated in terms of step numbers, total yields, costs, synthetic conditions and manufacturing safety. At last, the synthetic method of d6-elagolix was introduced. This review would be beneficial to the future process researches of elagolix and its deuterium analogues.
Synthesis of Elagolix
Recent Progress in the Synthesis of Elagolix
Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor

elagolix Preparation Products And Raw materials

Raw materials

4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]-, ethyl ester 3-[(2R)-2-Amino-2-phenylethyl]-5-(2-fluoro-3-methoxyphenyl)-1-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-6-methyl-2,4(1H,3H)-pyrimidinedione Methyl 4-bromobutyrate

Preparation Products

elagolix Suppliers

Global( 193)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
Exemed Pharmaceuticals (Oneiro Chemicals Pvt Ltd) +91-9687684674 +91-9099061028 Gujarat, India 30 58 Inquiry
KARPSCHEM LABORATORIES +91-7249203006 +91-7249203006 Maharashtra, India 786 58 Inquiry
CLEARSYNTH LABS LTD. +91-22-45045900 Hyderabad, India 6351 58 Inquiry
SynZeal Research Pvt Ltd +1 226-802-2078 Gujarat, India 6522 58 Inquiry
Beijing Hope Pharmaceutical Co., Ltd. +86-010-67886402 +8613611125266 China 71 58 Inquiry
Aladdin Scientific +1-+1(833)-552-7181 United States 52927 58 Inquiry
Hebei Yanxi Chemical Co., Ltd. +86-17531190177; +8617531190177 China 5873 58 Inquiry
Shaanxi Haibo Biotechnology Co., Ltd +undefined18602966907 China 1000 58 Inquiry
Capot Chemical Co.,Ltd. 571-85586718 +8613336195806 China 29798 60 Inquiry
Henan Tianfu Chemical Co.,Ltd. +86-0371-55170693 +86-19937530512 China 21667 55 Inquiry
Supplier Advantage
Exemed Pharmaceuticals (Oneiro Chemicals Pvt Ltd) 58
KARPSCHEM LABORATORIES 58
CLEARSYNTH LABS LTD. 58
SynZeal Research Pvt Ltd 58
Beijing Hope Pharmaceutical Co., Ltd. 58
Aladdin Scientific 58
Hebei Yanxi Chemical Co., Ltd. 58
Shaanxi Haibo Biotechnology Co., Ltd 58
Capot Chemical Co.,Ltd. 60
Henan Tianfu Chemical Co.,Ltd. 55

Related Qustion

834153-87-6(elagolix)Related Search:

(R)-2-(Boc-aMino)-2-phenylethyl 4-Methylbenzenesulfonate 1-[(1R)-2-hydroxy-1-phenylethyl]pyrrolidin-2-one Carbamic acid, N-[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]-, 1,1-dimethylethyl ester Elagolix Sodium 1-[2-fluoro-6-(trifluoromethyl)benzyl]-5-iodo-6-methylpyrimidine-2,4(1H,3H)-dione
Ganirelix Ganirelix Acetate Relugolix Abarelix Cetrorelix acetate
T-BUTYL 4-BROMOBUTYRATE 3-[(2R)-2-Amino-2-phenylethyl]-5-(2-fluoro-3-methoxyphenyl)-1-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-6-methyl-2,4(1H,3H)-pyrimidinedione 5-Bromo-1-(2-fluoro-6-trifluoromethyl-benzyl)-6-methyl-1H-pyrimidine-2,4-dione 2,2'-difluoro-3,3'-dimethoxy-1,1'-biphenyl Elagolix Sodium impurity4
1-(2-FLUORO-6-(TRIFLOROMETHYL)BENZYL)UREA 3-Bromo-2-fluoroanisole 5-(2-Fluoro-3-methoxyphenyl)-1-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-6-methyl-2,4(1H,3H)-pyrimidinedione
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elagolix 4-[[(1R)-2-[5-(2-Fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]butanoic acid Butanoic acid, 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]- 4-({(1R)-2-[5-(2-Fluoro-3-methoxyphenyl)-3-[2-fluoro-6-(trifluoromethyl)benzyl]-4-methyl-2,6-dioxo-3,6-dihydro-1(2H)-pyrimidinyl]-1-phenylethyl}amino)butanoic acid 4-[[(1R)-2-[5-(2-FLUORO-3-METHOXYPHENYL)-3-[[2-FLUORO-6-(TRIFLUOROMETHYL)PHENYL]METHYL]-4-METHYL-2,6-DIOXOPYRIMIDIN-1-YL]-1-PHENYLETHYL]AMINO]BUTANOIC ACID elagolix USP/EP/BP Seviram hydrochloride Elagolix (NBI-56418) CS-2011 CS-2232 Elagolix-004-R NBI 56418; NBI56418;NBI-56418 (R)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-[2-fluoro-6-(trifluoromethyl)benzyl]-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyric acid (R)-Elagolix ABT-620 Elagolix-d6 NBI 56418 (R)-4-((2-(5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)-1-phenylethyl)amino)butanoic acid Elagoli Elagolix Sodium Monomer Tropicamide Impurity 35 Elagolix sodium 4-[[(1R)-2-[5-(2-Fluoro-3-methoxyphenyl)-3-[[2-fluoro-6- (trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6- dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]butanoic acid Elagolix CAS 834153-87-6 C32H30F5N3O5 API