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HomeProductsActive Pharmaceutical IngredientsGonadotropin-Releasing Hormone Receptor (GnRHR) Elagolix Sodium 832720-36-2
Gonadotropin-Releasing Hormone Receptor (GnRHR) Elagolix Sodium 832720-36-2
  • Gonadotropin-Releasing Hormone Receptor (GnRHR) Elagolix Sodium 832720-36-2

Gonadotropin-Releasing Hormone Receptor (GnRHR) Elagolix Sodium 832720-36-2

    Unit Price: USD 1 / Gram
    Payment Type: T/T
    Incoterm: CIF
    Min. Order: 1 Gram
    Delivery Time: 15 Days

Basic Info

Model No.: 832720-36-2

Additional Info

Packaging: As Quantity

Productivity: As Order


Transportation: Air

Place of Origin: CHINA

Supply Ability: IN STOCK

Product Description

Elagolix Sodium CAS number is 832720-36-2, an oral gonadotropin-releasing hormone receptor antagonist, ultimately reduces blood levels of gonadal hormones by inhibiting the pituitary gland gonadotropin releasing hormone receptor. Elagolix Sodium was developed jointly by AbbVie and Neurocrine Biosciences. Aberdeen submitted the drug's NDA in September 2017, and was granted FDA priority review after more than one month, and was approved by the FDA on July 23, 2018 under the trade name Orilissa for therapeutic purposes. The pain caused by endometriosis and the first new oral drug for such indications in more than 10 years. Currently, Aberdeen is investigating the treatment of some sex hormone-mediated diseases such as uterine fibroids and endometriosis. So far, more than 40 clinical trials have been conducted, involving more than 3,000 patients. In addition, Phase III clinical trials of dysprosium in the treatment of uterine fibroids are also underway, with great market prospects.
There are two main methods for synthesizing the Elagolix Sodium in the literature: the first one: using 2-fluoro-6-trifluoromethylbenzonitrile as the raw material, first reducing the cyano group with borane, and then with urea in hydrochloric acid. Condensation to give 1-(2-fluoro-6-trifluoromethylphenethyl)urea intermediate, followed by cyclization with dipolyvinyl ketone to give the intermediate 1-[2-fluoro-6-(trifluoro Methyl)benzyl]-6-methylpyrimidine-2,4(1H,3H)-dione, which undergoes bromination, amine alkylation and then Suzuki with 2-fluoro-3-methoxybenzeneboronic acid The coupling reaction and acidolysis remove the Boc protecting group to obtain a key intermediate, and finally, condensation and hydrolysis with 4-bromo-n-butyric acid to obtain a final product. The linear step of this route is too long, the process is cumbersome, and the Suzuki coupling reaction with phenylboronic acid requires the use of tetrakis(triphenylphosphine)palladium, and the total yield of the route is low.
The second one is obtained by using ethyl 2-(2-fluoro-3-methoxyphenyl)formate as a raw material, and the intermediate obtained by sodium borohydride reduction and bromination reaction with acetonitrile is obtained by zinc powder. An enamine intermediate, which is then protected with phenyl carbonate and cyclized with (R)-tert-butyl(2-amino-1-phenethyl)aminocarbonate under a base to give the parent ring molecule, followed by benzyl The bromine intermediate completes the N-alkylation reaction to give the key intermediate of the vorage. Although this route greatly simplifies the reaction steps, the starting materials and intermediates are special and the raw material costs are high.
The synthesis of Elagolix Sodium 832720-36-2 is relatively long, some of which are difficult to react, and the impurities in the synthesis process are difficult to control. Therefore, it is necessary to strengthen the research on the process of Elagolix Sodium 832720-36-2.

Thera. Category:Antagonist

Cas No.:832720-36-2

Synonyms:Elagolix sodiuM;N4-{2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino}-butyrate;elagolix sodium salt;Elagolix sodiu;Evillagoli sodium;NBI-56418 sodium ;BI 56418NA;NBI 56418NA(elagolix na);

MF: C32H29F5N3NaO5



Assay: ≥99%

Packing:Export worthy packing

Material Safety Data Sheet:Available on request

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