TWI693208B - 惡拉戈利（elagolix）之製造方法 - Google Patents

惡拉戈利（elagolix）之製造方法 Download PDF

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Publication number
TWI693208B
TWI693208B TW107143337A TW107143337A TWI693208B TW I693208 B TWI693208 B TW I693208B TW 107143337 A TW107143337 A TW 107143337A TW 107143337 A TW107143337 A TW 107143337A TW I693208 B TWI693208 B TW I693208B
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TW
Taiwan
Prior art keywords
compound
reaction
preparation
oxagoli
added
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TW107143337A
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English (en)
Chinese (zh)
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TW201925159A (zh
Inventor
李丕旭
王鵬
谷向永
楊海龍
王中
蔣強華
劉遠華
夏輝
Original Assignee
大陸商蘇州鵬旭醫藥科技有限公司
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Priority claimed from CN201711263255.7A external-priority patent/CN109867631A/zh
Priority claimed from CN201810042494.8A external-priority patent/CN110128355A/zh
Priority claimed from CN201810941650.4A external-priority patent/CN110835302A/zh
Priority claimed from CN201811104129.1A external-priority patent/CN110938037A/zh
Application filed by 大陸商蘇州鵬旭醫藥科技有限公司 filed Critical 大陸商蘇州鵬旭醫藥科技有限公司
Publication of TW201925159A publication Critical patent/TW201925159A/zh
Application granted granted Critical
Publication of TWI693208B publication Critical patent/TWI693208B/zh

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J23/00—Catalysts comprising metals or metal oxides or hydroxides, not provided for in group B01J21/00
    • B01J23/38—Catalysts comprising metals or metal oxides or hydroxides, not provided for in group B01J21/00 of noble metals
    • B01J23/40—Catalysts comprising metals or metal oxides or hydroxides, not provided for in group B01J21/00 of noble metals of the platinum group metals
    • B01J23/44—Palladium
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J25/00—Catalysts of the Raney type
    • B01J25/02—Raney nickel
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C249/00—Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C249/04—Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of oximes
    • C07C249/08—Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of oximes by reaction of hydroxylamines with carbonyl compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/004—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reaction with organometalhalides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
    • C07D279/06—1,3-Thiazines; Hydrogenated 1,3-thiazines not condensed with other rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Materials Engineering (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
TW107143337A 2017-12-05 2018-12-04 惡拉戈利（elagolix）之製造方法 TWI693208B (zh)

Applications Claiming Priority (12)

Application Number Priority Date Filing Date Title
??201711263255.7 2017-12-05
CN201711263255.7A CN109867631A (zh) 2017-12-05 2017-12-05 一种含有6-甲基尿嘧啶结构化合物的制备方法
CN201711263255.7 2017-12-05
??201810042494.8 2018-01-17
CN201810042494.8A CN110128355A (zh) 2018-01-17 2018-01-17 一种含有6-甲基尿嘧啶结构化合物的制备方法
CN201810042494.8 2018-01-17
CN201811104129.1 2018-08-14
CN201810941650.4 2018-08-17
CN201810941650.4A CN110835302A (zh) 2018-08-17 2018-08-17 一种恶拉戈利及其钠盐的中间体及其制备方法
??201810941650.4 2018-08-17
CN201811104129.1A CN110938037A (zh) 2018-09-21 2018-09-21 一种依拉戈利钠盐药物中间体的制备方法
??201811104129.1 2018-09-21

Publications (2)

Publication Number Publication Date
TW201925159A TW201925159A (zh) 2019-07-01
TWI693208B true TWI693208B (zh) 2020-05-11

Family

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Family Applications (2)

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TW107143337A TWI693208B (zh) 2017-12-05 2018-12-04 惡拉戈利（elagolix）之製造方法
TW109111870A TW202030177A (zh) 2017-12-05 2018-12-04 惡拉戈利（elagolix）之製造方法

Family Applications After (1)

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TW109111870A TW202030177A (zh) 2017-12-05 2018-12-04 惡拉戈利（elagolix）之製造方法

Country Status (5)

Country Link
US (1) US11377426B2 (https=)
EP (1) EP3720845A4 (https=)
JP (1) JP7200261B2 (https=)
TW (2) TWI693208B (https=)
WO (1) WO2019112968A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7200261B2 (ja) 2017-12-05 2023-01-06 スージョウ ポンシュー ファーマテック カンパニー リミテッド エラゴリクスを作製するプロセス
BR112021000973A2 (pt) * 2018-07-23 2021-04-20 Abbvie Inc. composições e processos de sódio de elagolix
ES2802815B2 (es) 2019-07-12 2022-03-14 Moehs Iberica Sl Sal clorhidrato de 3-[2(r)-amino-2-feniletil]-5-(2-fluoro-3-metoxifenil)-1-[2-fluoro-6-(trifluorometil)bencil]-6-metil-1h-pirimidin-2,4(1h,3h)-diona (i) en forma solida, procedimiento para su preparacion y uso de la misma en la sintesis de elagolix
TWI755055B (zh) * 2019-09-18 2022-02-11 台灣神隆股份有限公司 用於製備惡拉戈利鈉及其中間體的方法
CN116283797B (zh) * 2022-12-30 2024-11-29 浙江车头制药股份有限公司 一种噁拉戈利钠的合成方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5977414A (en) * 1996-07-30 1999-11-02 Nippon Soda Co., Ltd. 2,3-Dihalogeno-6-trifluoromethylbenzene derivatives and processes for the preparation thereof
US20050131032A1 (en) * 2002-02-08 2005-06-16 Sing-Yuen Sit (Oxime)carbamoyl fatty acid amide hydrolase inhibitors
US7419983B2 (en) * 2003-07-07 2008-09-02 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods related thereto
US20120059179A1 (en) * 2009-04-03 2012-03-08 The Scripps Research Insitiute Palladium-catalyzed ortho-fluorination
US20170320836A1 (en) * 2007-11-07 2017-11-09 Helen Chou Processes for the preparation of uracil derivatives

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0711521D0 (en) 2007-06-14 2007-07-25 Glaxo Group Ltd Novel compounds
AU2016229268B2 (en) 2015-03-06 2020-09-10 Pharmakea, Inc. Fluorinated lysyl oxidase-like 2 inhibitors and uses thereof
JP7200261B2 (ja) 2017-12-05 2023-01-06 スージョウ ポンシュー ファーマテック カンパニー リミテッド エラゴリクスを作製するプロセス

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5977414A (en) * 1996-07-30 1999-11-02 Nippon Soda Co., Ltd. 2,3-Dihalogeno-6-trifluoromethylbenzene derivatives and processes for the preparation thereof
US20050131032A1 (en) * 2002-02-08 2005-06-16 Sing-Yuen Sit (Oxime)carbamoyl fatty acid amide hydrolase inhibitors
US7419983B2 (en) * 2003-07-07 2008-09-02 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods related thereto
US20170320836A1 (en) * 2007-11-07 2017-11-09 Helen Chou Processes for the preparation of uracil derivatives
US20120059179A1 (en) * 2009-04-03 2012-03-08 The Scripps Research Insitiute Palladium-catalyzed ortho-fluorination

Also Published As

Publication number Publication date
JP2021505683A (ja) 2021-02-18
WO2019112968A1 (en) 2019-06-13
US20210214318A1 (en) 2021-07-15
US11377426B2 (en) 2022-07-05
JP7200261B2 (ja) 2023-01-06
TW201925159A (zh) 2019-07-01
EP3720845A4 (en) 2021-09-01
EP3720845A1 (en) 2020-10-14
TW202030177A (zh) 2020-08-16

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