EA201991507A1 - Улучшенный способ получения гидрохлорида (r)-6-гидрокси-8-[1-гидрокси-2-[2-(4-метоксифенил)-1,1-диметил]этиламиноэтил]-2h-1,4-бензоксазин-3(4h)-она - Google Patents

Улучшенный способ получения гидрохлорида (r)-6-гидрокси-8-[1-гидрокси-2-[2-(4-метоксифенил)-1,1-диметил]этиламиноэтил]-2h-1,4-бензоксазин-3(4h)-она

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Publication number
EA201991507A1
EA201991507A1 EA201991507A EA201991507A EA201991507A1 EA 201991507 A1 EA201991507 A1 EA 201991507A1 EA 201991507 A EA201991507 A EA 201991507A EA 201991507 A EA201991507 A EA 201991507A EA 201991507 A1 EA201991507 A1 EA 201991507A1
Authority
EA
Eurasian Patent Office
Prior art keywords
hydroxy
methoxyphenyl
dimethyl
ethylaminoethyl
benzoxaszin
Prior art date
Application number
EA201991507A
Other languages
English (en)
Inventor
Энрик Капдевила Урбанеха
Хуан Юге Клоте
Пере Дальмасес Бархоан
Original Assignee
Инке, С.А.
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 Инке, С.А. filed Critical Инке, С.А.
Priority claimed from PCT/EP2017/083444 external-priority patent/WO2018114887A1/en
Publication of EA201991507A1 publication Critical patent/EA201991507A1/ru

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235Saturated compounds containing more than one carboxyl group
    • C07C59/245Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255Tartaric acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/02Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/54Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C217/56Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms
    • C07C217/60Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/07Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/341,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/361,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/56Ring systems containing bridged rings
    • C07C2603/58Ring systems containing bridged rings containing three rings
    • C07C2603/60Ring systems containing bridged rings containing three rings containing at least one ring with less than six members
    • C07C2603/66Ring systems containing bridged rings containing three rings containing at least one ring with less than six members containing five-membered rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Настоящее изобретение относится к улучшенному способу получения (R)-6-гидрокси-8-[1-гидрокси-2-[2-(4-метоксифенил)-1,1-диметил]этиламиноэтил]-2H-1,4-бензоксазин-3(4H)-она с высокой чистотой и высоким выходом путем применения L-тартрата 1,1-диметил-2-(4-метоксифенил)этиламина, малеата 1,1-диметил-2-(4-метоксифенил)этиламина или камфорсульфонатной соли промежуточного продукта (4). Настоящее изобретение также относится к указанным солям, к способам их получения и к их применению для получения (R)-6-гидрокси-8-[1-гидрокси-2-[2-(4-метоксифенил)-1,1-диметил]этиламиноэтил]-2H-1,4-бензоксазин-3(4H)-она или его фармацевтически приемлемой соли.
EA201991507A 2017-07-10 2017-12-19 Улучшенный способ получения гидрохлорида (r)-6-гидрокси-8-[1-гидрокси-2-[2-(4-метоксифенил)-1,1-диметил]этиламиноэтил]-2h-1,4-бензоксазин-3(4h)-она EA201991507A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP17382449 2017-07-10
PCT/EP2017/083444 WO2018114887A1 (en) 2016-12-20 2017-12-19 Improved process for the manufacture of r-6-hydroxy-8-[1-hydroxy-2-[2-(4-methoxyphenyl)-1,1-dimethylethylaminoethyl]-2h-1,4-benzoxazin-3(4h)-one hydrochloride

Publications (1)

Publication Number Publication Date
EA201991507A1 true EA201991507A1 (ru) 2020-01-21

Family

ID=59315559

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201991507A EA201991507A1 (ru) 2017-07-10 2017-12-19 Улучшенный способ получения гидрохлорида (r)-6-гидрокси-8-[1-гидрокси-2-[2-(4-метоксифенил)-1,1-диметил]этиламиноэтил]-2h-1,4-бензоксазин-3(4h)-она

Country Status (2)

Country Link
EA (1) EA201991507A1 (ru)
PT (1) PT3558954T (ru)

Also Published As

Publication number Publication date
PT3558954T (pt) 2022-03-07

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