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EA201201127A1 - Способ получения небиволола - Google Patents

Способ получения небиволола

Info

Publication number
EA201201127A1
EA201201127A1 EA201201127A EA201201127A EA201201127A1 EA 201201127 A1 EA201201127 A1 EA 201201127A1 EA 201201127 A EA201201127 A EA 201201127A EA 201201127 A EA201201127 A EA 201201127A EA 201201127 A1 EA201201127 A1 EA 201201127A1
Authority
EA
Eurasian Patent Office
Prior art keywords
nebivolol
obtaining
reduced
diastereoisomers
themselves
Prior art date
Application number
EA201201127A
Other languages
English (en)
Other versions
EA019691B1 (ru
Inventor
Сандра Бартоли
Амалия Чиполлоне
Даниэла Фаттори
Original Assignee
Менарини Интернешнл Оперейшнз Люксембург 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 Менарини Интернешнл Оперейшнз Люксембург С.А. filed Critical Менарини Интернешнл Оперейшнз Люксембург С.А.
Publication of EA201201127A1 publication Critical patent/EA201201127A1/ru
Publication of EA019691B1 publication Critical patent/EA019691B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
    • C07D311/60—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4 with aryl radicals attached in position 2

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Steroid Compounds (AREA)
  • Treating Waste Gases (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Saccharide Compounds (AREA)
  • Treatment Of Liquids With Adsorbents In General (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Настоящее изобретение относится к новому способу синтеза небиволола, представленному на схеме (1), и уменьшенному сокращенному числу стадий, характеризующихся высокими выходами, отличающемуся кинетическим разделением двух эпоксидных пар диастереоизомеров между собой (смесь 1), позволяющим избежать сложных хроматографических разделений.
EA201201127A 2010-02-11 2011-02-09 Способ получения небиволола EA019691B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ITRM2010A000053A IT1397962B1 (it) 2010-02-11 2010-02-11 Processo per la preparazione del nebivololo.
PCT/EP2011/051876 WO2011098474A1 (en) 2010-02-11 2011-02-09 Process for the preparation of nebivolol

Publications (2)

Publication Number Publication Date
EA201201127A1 true EA201201127A1 (ru) 2013-01-30
EA019691B1 EA019691B1 (ru) 2014-05-30

Family

ID=42289104

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201201127A EA019691B1 (ru) 2010-02-11 2011-02-09 Способ получения небиволола

Country Status (22)

Country Link
US (1) US8487122B2 (ru)
EP (1) EP2534142B1 (ru)
JP (1) JP5698266B2 (ru)
KR (1) KR101726468B1 (ru)
CN (1) CN102858759B (ru)
AR (1) AR080149A1 (ru)
AU (1) AU2011214396B2 (ru)
BR (1) BR112012020252B8 (ru)
CA (1) CA2786833C (ru)
EA (1) EA019691B1 (ru)
ES (1) ES2445543T3 (ru)
HK (1) HK1179626A1 (ru)
HR (1) HRP20140155T1 (ru)
IL (1) IL220846A (ru)
IT (1) IT1397962B1 (ru)
MX (1) MX2012009386A (ru)
PL (1) PL2534142T3 (ru)
PT (1) PT2534142E (ru)
RS (1) RS53134B (ru)
SG (1) SG183266A1 (ru)
WO (1) WO2011098474A1 (ru)
ZA (1) ZA201206221B (ru)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8785664B2 (en) * 2010-02-11 2014-07-22 Menarini International Operations Luxembourg S.A. Process for the preparation of nebivolol
ITRM20110418A1 (it) 2011-08-02 2013-02-03 Menarini Int Operations Lu Sa Processo per la preparazione di epossidi quali intermedi per la sintesi del nebivololo.
CN104650022B (zh) * 2013-11-20 2018-09-25 浙江奥翔药业股份有限公司 奈必洛尔的合成方法及其中间体化合物
MX354930B (es) * 2014-10-23 2018-03-20 Consorcio Comex S A De C V Composicion para aerosol usada para marcar o delimitar en cualquier tipo de superficie con una duracion temporal.
JP6921913B2 (ja) * 2015-05-19 2021-08-18 チョーチアン オウスン ファーマシューティカル カンパニー リミテッド ネビボロールの合成方法及びその中間化合物
ES2901966T3 (es) * 2015-05-19 2022-03-24 Zhejiang Ausun Pharmaceutical Co Ltd Método de síntesis de nebivolol y compuesto intermedio del mismo
CN105085499B (zh) * 2015-08-07 2018-09-25 上海现代制药海门有限公司 盐酸奈必洛尔中间体混合物的结晶分离方法
ITUB20160227A1 (it) * 2016-01-21 2017-07-21 Menarini Int Operations Luxembourg Sa Processo per la sintesi di intermedi di Nebivololo

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2475298A1 (fr) * 1980-02-01 1981-08-07 Thomson Csf Cellule photovoltaique et pile solaire utilisant une telle cellule
US4654362A (en) * 1983-12-05 1987-03-31 Janssen Pharmaceutica, N.V. Derivatives of 2,2'-iminobisethanol
CA1337429C (en) 1983-12-05 1995-10-24 Guy Rosalia Eugene Van Lommen Derivatives of 2,2'-iminobisethanol
CA1337432C (en) * 1988-03-23 1995-10-24 Raymond M. Xhonneux Method of lowering the blood pressure
US6545040B1 (en) 1988-03-23 2003-04-08 Janssen Pharmaceutica N.V. Method of lowering the blood pressure
DE3809857A1 (de) 1988-03-24 1989-10-05 Philips Patentverwaltung Blasformmaschine zum blasformen von hohlkoerpern mit polsterregelung
TW355683B (en) 1994-02-17 1999-04-11 Janssen Pharmaceutica Nv Composition containing micronized nebivolol
HU227236B1 (en) * 2002-11-06 2010-12-28 Egis Gyogyszergyar Nyilvanosan Muekoedoe Reszvenytarsasag New process for the production of racemic and the pure [2s[2r*[r[r*]]]]-and [2r[2s*[s[s*]]]]-enantiomers of nebivolol
EP1737847B1 (en) * 2004-07-30 2008-06-04 Torrent Pharmaceuticals Ltd Nebivolol and its pharmaceutically acceptable salts, process for preparation and pharmaceutical compositions of nebivolol
UA87155C2 (ru) 2004-08-13 2009-06-25 Хардор Меканизм Продакшн Лтд Машина для обёртывание профилей
AT502220A1 (de) * 2005-07-19 2007-02-15 Pharmacon Forschung & Beratung Verfahren zur herstellung von nebivolol
WO2007041805A1 (en) 2005-10-13 2007-04-19 Burns Bay Investments Pty Ltd Elongate lighting means
US7560575B2 (en) * 2005-12-28 2009-07-14 Acino Pharma Ag Process for preparation of racemic Nebivolol
EP1803716B1 (en) 2005-12-28 2012-07-25 Acino Pharma AG A process for preparation of racemic nebivolol
US7858812B2 (en) 2006-01-18 2010-12-28 Hetero Drugs Limited Process for isolation of desired isomers of nebivolol intermediates
PL2099790T3 (pl) 2006-11-27 2010-12-31 Zach System Spa Sposób wytwarzania nebiwololu
SI2102196T1 (sl) 2006-11-27 2012-12-31 Zach System S.P.A. Postopek za pripravo nebivolola
CN101235024A (zh) * 2008-02-01 2008-08-06 中国科学院上海有机化学研究所 一类苯并二氢吡喃类化合物、合成方法和用途

Also Published As

Publication number Publication date
US8487122B2 (en) 2013-07-16
PT2534142E (pt) 2014-02-24
EP2534142A1 (en) 2012-12-19
PL2534142T3 (pl) 2014-05-30
ITRM20100053A1 (it) 2011-08-12
EA019691B1 (ru) 2014-05-30
IL220846A0 (en) 2012-08-30
AR080149A1 (es) 2012-03-14
WO2011098474A1 (en) 2011-08-18
CA2786833A1 (en) 2011-08-18
JP5698266B2 (ja) 2015-04-08
IL220846A (en) 2014-12-31
CA2786833C (en) 2017-03-07
BR112012020252B8 (pt) 2021-05-25
CN102858759B (zh) 2015-12-16
KR20120129952A (ko) 2012-11-28
JP2013519647A (ja) 2013-05-30
EP2534142B1 (en) 2013-11-27
HRP20140155T1 (hr) 2014-03-14
MX2012009386A (es) 2012-09-12
HK1179626A1 (en) 2013-10-04
IT1397962B1 (it) 2013-02-04
US20120316351A1 (en) 2012-12-13
AU2011214396B2 (en) 2014-06-05
KR101726468B1 (ko) 2017-04-12
SG183266A1 (en) 2012-09-27
AU2011214396A1 (en) 2012-10-04
ZA201206221B (en) 2014-01-29
RS53134B (en) 2014-06-30
BR112012020252A2 (pt) 2016-08-09
ES2445543T3 (es) 2014-03-03
BR112012020252B1 (pt) 2021-05-04
CN102858759A (zh) 2013-01-02

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Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ KG MD TJ TM