SG11201403216UA - Methods and compounds useful in the synthesis of orexin-2 receptor antagonists - Google Patents

Methods and compounds useful in the synthesis of orexin-2 receptor antagonists

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Publication number
SG11201403216UA
SG11201403216UA SG11201403216UA SG11201403216UA SG11201403216UA SG 11201403216U A SG11201403216U A SG 11201403216UA SG 11201403216U A SG11201403216U A SG 11201403216UA SG 11201403216U A SG11201403216U A SG 11201403216UA SG 11201403216U A SG11201403216U A SG 11201403216UA
Authority
SG
Singapore
Prior art keywords
tsukuba
eisai
chome
tokodai
shi
Prior art date
Application number
SG11201403216UA
Other languages
English (en)
Inventor
George Anthony Moniz
Annie Zhu Wilcoxen
Farid Benayoud
Jaemoon Lee
Huiming Zhang
Taro Terauchi
Ayumi Takemura
Yu Yoshida
Toshiaki Tanaka
Keiichi Sorimachi
Yoshimitsu Naoe
Yuji Kazuta
Original Assignee
Eisai R&D Man Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Eisai R&D Man Co Ltd filed Critical Eisai R&D Man Co Ltd
Publication of SG11201403216UA publication Critical patent/SG11201403216UA/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63Esters of sulfonic acids
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/26Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/42Separation; Purification; Stabilisation; Use of additives
    • C07C303/44Separation; Purification
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63Esters of sulfonic acids
    • C07C309/64Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/65Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • C07C309/66Methanesulfonates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D239/34One oxygen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P7/00Preparation of oxygen-containing organic compounds
    • C12P7/02Preparation of oxygen-containing organic compounds containing a hydroxy group
    • C12P7/22Preparation of oxygen-containing organic compounds containing a hydroxy group aromatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/02Systems containing only non-condensed rings with a three-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C33/00Unsaturated compounds having hydroxy or O-metal groups bound to acyclic carbon atoms
    • C07C33/36Polyhydroxylic alcohols containing six-membered aromatic rings and other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00Preparation of carboxylic acid esters
    • C07C67/03Preparation of carboxylic acid esters by reacting an ester group with a hydroxy group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/02Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
    • C07C69/12Acetic acid esters
    • C07C69/16Acetic acid esters of dihydroxylic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Wood Science & Technology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Microbiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • General Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (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)
  • Steroid Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
SG11201403216UA 2012-02-17 2013-02-14 Methods and compounds useful in the synthesis of orexin-2 receptor antagonists SG11201403216UA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261600109P 2012-02-17 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

Publications (1)

Publication Number Publication Date
SG11201403216UA true SG11201403216UA (en) 2014-12-30

Family

ID=47755050

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201403216UA SG11201403216UA (en) 2012-02-17 2013-02-14 Methods and compounds useful in the synthesis of orexin-2 receptor antagonists

Country Status (13)

Country Link
US (3) US9416109B2 (enrdf_load_stackoverflow)
EP (1) EP2814798B1 (enrdf_load_stackoverflow)
JP (1) JP6147279B2 (enrdf_load_stackoverflow)
CN (1) CN104114524B (enrdf_load_stackoverflow)
BR (1) BR112014019909B1 (enrdf_load_stackoverflow)
CA (1) CA2861493C (enrdf_load_stackoverflow)
ES (1) ES2733750T3 (enrdf_load_stackoverflow)
HU (1) HUE043995T2 (enrdf_load_stackoverflow)
IL (1) IL232949A (enrdf_load_stackoverflow)
MX (1) MX352881B (enrdf_load_stackoverflow)
RU (1) RU2617696C2 (enrdf_load_stackoverflow)
SG (1) SG11201403216UA (enrdf_load_stackoverflow)
WO (1) WO2013123240A1 (enrdf_load_stackoverflow)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
NZ628491A (en) 2012-02-07 2016-06-24 Eolas Therapeutics Inc Substituted prolines / piperidines as orexin receptor antagonists
US9416109B2 (en) * 2012-02-17 2016-08-16 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
US10221170B2 (en) 2014-08-13 2019-03-05 Eolas Therapeutics, Inc. Difluoropyrrolidines as orexin receptor modulators
CN109219606B (zh) 2016-02-12 2021-10-01 阿斯利康(瑞典)有限公司 食欲素受体调节剂的卤素取代的哌啶
CN110799501B (zh) * 2017-08-01 2022-11-22 博健制药有限责任公司 一种食欲素受体拮抗剂的晶型及其制备方法和用途
GB201807898D0 (en) * 2018-05-15 2018-06-27 Kancera Ab New processes and products with increased chiral purity
JP7384810B2 (ja) * 2018-09-07 2023-11-21 住友化学株式会社 シクロプロパン化合物の製造方法
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
WO2020249689A1 (en) 2019-06-12 2020-12-17 Nouryon Chemicals International B.V. Process for the production of peroxyesters
HUE063677T2 (hu) 2019-06-12 2024-01-28 Nouryon Chemicals Int Bv Eljárás diacil-peroxidok elõállítására
JP7355858B2 (ja) * 2019-06-12 2023-10-03 ヌーリオン ケミカルズ インターナショナル ベスローテン フェノーツハップ 水性側流からカルボン酸を単離するための方法
JP7336541B2 (ja) 2019-06-12 2023-08-31 ヌーリオン ケミカルズ インターナショナル ベスローテン フェノーツハップ 過酸化ジアシルを生成するためのプロセス
HUE063796T2 (hu) 2019-06-12 2024-01-28 Nouryon Chemicals Int Bv Eljárás diacil-peroxidok elõállítására
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
CA3165481A1 (en) 2019-12-20 2021-06-24 Eisai R&D Management Co., Ltd. Use of lemborexant for treating insomnia
EP4059504A4 (en) 2020-01-16 2023-12-27 Eisai R&D Management Co., Ltd. LEMBOREXANT MEDICINAL COMPOSITION AND MEDICAL COMPOSITION CONTAINING SAME
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
CN118843622A (zh) * 2022-03-25 2024-10-25 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
WO2023178693A1 (zh) * 2022-03-25 2023-09-28 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
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
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

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2302994A1 (fr) * 1975-03-06 1976-10-01 Fabre Sa Pierre Procede de preparation d'acides aryl-1, hydroxy methyl-2 cyclopropanes carboxyliques et de leurs lactones utiles comme intermediaires de synthese dans l'industrie pharmaceutique
US5849954A (en) * 1996-01-18 1998-12-15 Research Corporation Technologies, Inc. Method of peptide synthesis
WO2004037212A2 (en) 2002-10-24 2004-05-06 Sepracor, Inc. Compositions comprising zopiclone derivatives and methods of making and using the same
US8138377B2 (en) 2006-11-07 2012-03-20 Dov Pharmaceutical, Inc. Arylbicyclo[3.1.0]hexylamines and methods and compositions for their preparation and use
US8242121B2 (en) * 2007-05-23 2012-08-14 Merck Sharp & Dohme Corp. Pyridyl piperidine orexin receptor antagonists
EP2150115B1 (en) * 2007-05-23 2013-09-18 Merck Sharp & Dohme Corp. Cyclopropyl pyrrolidine orexin receptor antagonists
EA201100368A1 (ru) 2008-09-18 2011-12-30 Пфайзер Лимитед Амидные соединения, полезные в терапии
EP2370427A1 (en) 2008-12-02 2011-10-05 Glaxo Group Limited N-{[(ir,4s,6r-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and uses thereof
FR2941454B1 (fr) * 2009-01-29 2011-04-01 Pf Medicament Proced de synthese du (1s,2r)-milnacipran
US8101643B2 (en) 2009-02-27 2012-01-24 Enanta Pharmaceuticals, Inc. Benzimidazole derivatives
US9340752B2 (en) 2009-03-09 2016-05-17 Novozymes A/S Enzymatic removal of steryl glycosides in fatty acid alkyl esters
PL2626350T3 (pl) * 2010-09-22 2015-08-31 Eisai R&D Man Co Ltd Związek cyklopropanu
US9416109B2 (en) * 2012-02-17 2016-08-16 Eisai R&D Management Co., Ltd. Methods and compounds useful in the synthesis of orexin-2 receptor antagonists

Also Published As

Publication number Publication date
US9416109B2 (en) 2016-08-16
US20180044285A1 (en) 2018-02-15
CA2861493C (en) 2019-09-24
IL232949A (en) 2016-08-31
CN104114524A (zh) 2014-10-22
CA2861493A1 (en) 2013-08-22
BR112014019909A8 (pt) 2017-07-11
US9828336B2 (en) 2017-11-28
BR112014019909A2 (enrdf_load_stackoverflow) 2017-06-20
US20150025237A1 (en) 2015-01-22
CN104114524B (zh) 2016-08-17
IL232949A0 (en) 2014-08-03
MX352881B (es) 2017-12-13
ES2733750T3 (es) 2019-12-02
WO2013123240A1 (en) 2013-08-22
US20160318858A1 (en) 2016-11-03
RU2014137470A (ru) 2016-04-10
JP2015509939A (ja) 2015-04-02
HUE043995T2 (hu) 2019-09-30
EP2814798B1 (en) 2019-04-03
JP6147279B2 (ja) 2017-06-14
BR112014019909B1 (pt) 2020-01-28
RU2617696C2 (ru) 2017-04-26
MX2014009917A (es) 2014-11-13
EP2814798A1 (en) 2014-12-24

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