엘라골릭스

한글명:엘라골릭스

카스 번호834153-87-6

상품명:elagolix

CBNumberCB51518509

분자식C32H30F5N3O5

포뮬러 무게631.59

MOL 파일834153-87-6.mol

동의어(한글)

엘라골릭스

화학적 성질

끓는 점	728.6±70.0 °C(Predicted)
밀도	1.350
저장 조건	Store at -20°C
용해도	DMSO : ≥ 100 mg/mL (158.33 mM)
산도 계수 (pKa)	4.40±0.10(Predicted)
물리적 상태	Solid
색상	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

그림문자(GHS)

엘라골릭스 화학적 특성, 용도, 생산

개요
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.
용도
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.
제조 방법
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.

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

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