CN104114524B - 用于食欲肽-2受体拮抗剂的合成的方法和化合物 - Google Patents

用于食欲肽-2受体拮抗剂的合成的方法和化合物 Download PDF

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CN104114524B
CN104114524B CN201380009575.3A CN201380009575A CN104114524B CN 104114524 B CN104114524 B CN 104114524B CN 201380009575 A CN201380009575 A CN 201380009575A CN 104114524 B CN104114524 B CN 104114524B
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CN104114524A (zh
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G.A.莫尼斯
A.Z.威尔科克森
F.贝纳尤德
李在文
张慧明
寺内太朗
竹村鲇美
吉田融
田中利知
反町启
反町启一
直江吉充
数田雄二
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Sanitary Material R&d Management Co ltd
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    • C07C29/00Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring
    • C07C29/132Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by reduction of an oxygen containing functional group
    • C07C29/136Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by reduction of an oxygen containing functional group of >C=O containing groups, e.g. —COOH
    • C07C29/147Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by reduction of an oxygen containing functional group of >C=O containing groups, e.g. —COOH of carboxylic acids or derivatives thereof
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    • C07C303/00Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
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    • C07C303/28Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids by reaction of hydroxy compounds with sulfonic acids or derivatives thereof
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    • C07C303/00Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
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    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
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    • C07C309/64Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
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    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C12P7/00Preparation of oxygen-containing organic compounds
    • C12P7/02Preparation of oxygen-containing organic compounds containing a hydroxy group
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    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
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    • C07C309/72Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/73Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
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    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82Benzo [b] furans; Hydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/83Oxygen atoms

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  • Chemical & Material Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Microbiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Furan Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201380009575.3A 2012-02-17 2013-02-14 用于食欲肽-2受体拮抗剂的合成的方法和化合物 Active CN104114524B (zh)

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US201261600109P 2012-02-17 2012-02-17
US61/600109 2012-02-17
US61/600,109 2012-02-17
PCT/US2013/026204 WO2013123240A1 (en) 2012-02-17 2013-02-14 Methods and compounds useful in the synthesis of orexin-2 receptor antagonists

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US (3) US9416109B2 (enExample)
EP (1) EP2814798B1 (enExample)
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BR (1) BR112014019909B1 (enExample)
CA (1) CA2861493C (enExample)
ES (1) ES2733750T3 (enExample)
HU (1) HUE043995T2 (enExample)
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Cited By (6)

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EP3983340B1 (en) * 2019-06-12 2023-08-02 Nouryon Chemicals International B.V. Method for isolating carboxylic acid from an aqueous side stream
US11976034B2 (en) 2019-06-12 2024-05-07 Nouryon Chemicals International B.V. Process for the production of diacyl peroxides
US11976035B2 (en) 2019-06-12 2024-05-07 Nouryon Chemicals International B.V. Process for the production of diacyl peroxides
US12209065B2 (en) 2019-06-12 2025-01-28 Nouryon Chemicals International B.V. Process for the production of diacyl peroxides
US12215074B2 (en) 2019-06-12 2025-02-04 Nouryon Chemicals International B.V. Process for the production of peroxyesters
CN119930526A (zh) * 2025-04-07 2025-05-06 东北制药集团股份有限公司 一种莱博雷生中间体的制备方法

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ES2672732T3 (es) 2012-02-07 2018-06-15 Eolas Therapeutics Inc. Prolinas/piperidinas sustituidas como antagonistas del receptor de orexina
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
WO2013123240A1 (en) * 2012-02-17 2013-08-22 Eisai R&D Management Co., Ltd Methods and compounds useful in the synthesis of orexin-2 receptor antagonists
RU2681937C2 (ru) 2014-08-06 2019-03-14 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Способ получения пиримидин-1-олового соединения и его промежуточного соединения
UY36272A (es) 2014-08-13 2016-02-29 Eolas Therapeutics Inc Difluoropirrolidinas como moduladores de los receptores de orexinas
TWI710557B (zh) 2016-02-12 2020-11-21 美商伊歐拉斯治療學公司 作為食慾素受體調節劑之經鹵素取代之六氫吡啶
JP7179049B2 (ja) * 2017-08-01 2022-11-28 ベルゲン ファーマシューティカル、 エルエルシー オレキシン受容体拮抗薬の結晶形及びその製造方法並びに用途
GB201807898D0 (en) * 2018-05-15 2018-06-27 Kancera Ab New processes and products with increased chiral purity
US12098137B2 (en) 2018-09-07 2024-09-24 Sumitomo Chemical Company, Limited Method for manufacturing cyclopropane compound
ES3013667T3 (en) * 2019-05-15 2025-04-14 Eisai R&D Man Co Ltd Method and compound useful in preparation of orexin-2 receptor antagonist, and lemborexant having few impurities
WO2020263253A1 (en) * 2019-06-26 2020-12-30 Moline Margaret Lemborexant for treating sleep issues
WO2021119223A1 (en) 2019-12-11 2021-06-17 Teva Czech Industries S.R.O. Solid state form of lemborexant
JP2023508011A (ja) 2019-12-20 2023-02-28 エーザイ・アール・アンド・ディー・マネジメント株式会社 不眠症を治療するためのレンボレキサントの使用
JPWO2021145373A1 (enExample) 2020-01-16 2021-07-22
ES2933074B2 (es) * 2021-07-26 2023-09-29 Moehs Iberica Sl Procedimiento de sintesis de 2,4-dimetilpirimidin-5-ol, nuevos intermedios de dicho procedimiento y uso del producto en la sintesis de lemborexant
CN118871427A (zh) * 2022-03-25 2024-10-29 浙江华海药业股份有限公司 一种莱博雷生及其中间体的制备方法
WO2023178702A1 (zh) * 2022-03-25 2023-09-28 浙江华海药业股份有限公司 莱博雷生及其中间体化合物的制备方法
CN114778745B (zh) * 2022-06-21 2022-09-16 南京威凯尔生物医药科技有限公司 一种高效液相色谱法检测仑布雷生中间体及其对映体杂质的方法

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Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3983340B1 (en) * 2019-06-12 2023-08-02 Nouryon Chemicals International B.V. Method for isolating carboxylic acid from an aqueous side stream
US11976034B2 (en) 2019-06-12 2024-05-07 Nouryon Chemicals International B.V. Process for the production of diacyl peroxides
US11976035B2 (en) 2019-06-12 2024-05-07 Nouryon Chemicals International B.V. Process for the production of diacyl peroxides
US12209065B2 (en) 2019-06-12 2025-01-28 Nouryon Chemicals International B.V. Process for the production of diacyl peroxides
US12215074B2 (en) 2019-06-12 2025-02-04 Nouryon Chemicals International B.V. Process for the production of peroxyesters
CN119930526A (zh) * 2025-04-07 2025-05-06 东北制药集团股份有限公司 一种莱博雷生中间体的制备方法
CN119930526B (zh) * 2025-04-07 2025-07-08 东北制药集团股份有限公司 一种莱博雷生中间体的制备方法

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US9416109B2 (en) 2016-08-16
EP2814798A1 (en) 2014-12-24
MX352881B (es) 2017-12-13
BR112014019909A8 (pt) 2017-07-11
CA2861493C (en) 2019-09-24
US20150025237A1 (en) 2015-01-22
MX2014009917A (es) 2014-11-13
BR112014019909A2 (enExample) 2017-06-20
US20160318858A1 (en) 2016-11-03
HUE043995T2 (hu) 2019-09-30
SG11201403216UA (en) 2014-12-30
JP6147279B2 (ja) 2017-06-14
JP2015509939A (ja) 2015-04-02
WO2013123240A1 (en) 2013-08-22
US20180044285A1 (en) 2018-02-15
CN104114524A (zh) 2014-10-22
IL232949A0 (en) 2014-08-03
BR112014019909B1 (pt) 2020-01-28
EP2814798B1 (en) 2019-04-03
US9828336B2 (en) 2017-11-28
RU2617696C2 (ru) 2017-04-26
IL232949A (en) 2016-08-31
ES2733750T3 (es) 2019-12-02
RU2014137470A (ru) 2016-04-10
CA2861493A1 (en) 2013-08-22

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