HRP20110796T1 - Postupak dobivanja - Google Patents

Postupak dobivanja Download PDF

Info

Publication number
HRP20110796T1
HRP20110796T1 HR20110796T HRP20110796T HRP20110796T1 HR P20110796 T1 HRP20110796 T1 HR P20110796T1 HR 20110796 T HR20110796 T HR 20110796T HR P20110796 T HRP20110796 T HR P20110796T HR P20110796 T1 HRP20110796 T1 HR P20110796T1
Authority
HR
Croatia
Prior art keywords
reaction
solvent
mixture
carried out
process according
Prior art date
Application number
HR20110796T
Other languages
English (en)
Inventor
Berwe Mathias
Thomas Christian
Rehse Joachim
Grotjohann Dirk
Original Assignee
Bayer Pharma Aktiengesellschaft
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34716548&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20110796(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Pharma Aktiengesellschaft filed Critical Bayer Pharma Aktiengesellschaft
Publication of HRP20110796T1 publication Critical patent/HRP20110796T1/hr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

Postupak za dobivanje 5-kloro-N-({(5S)-2-okso-3-[4-(3-okso-4-morfolinil)fenil]-1,3-oksazolidin-5-il}metil)-2- tiofenkarboksamida sa formulom (I) sa reakcijom 4-{4-[(5S)-5-(aminometil)-2-okso-1,3-oksazolidin-3-il]fenil}morfolin-3-on (VII) hidroklorida sa 5-klorotiofen-2- karbonil kloridom (IV), naznačen time da se reakcija provodi u otapalu odabranom iz skupine koja sadrži eter, alkohol, keton i vodu ili u njihovoj mješavini uz uporabu anorganske baze. Patent sadrži još 12 patentnih zahtjeva.

Claims (13)

1. Postupak za dobivanje 5-kloro-N-({(5S)-2-okso-3-[4-(3-okso-4-morfolinil)fenil]-1,3-oksazolidin-5-il}metil)-2- tiofenkarboksamida sa formulom (I) sa reakcijom 4-{4-[(5S)-5-(aminometil)-2-okso-1,3-oksazolidin-3-il]fenil}morfolin-3-on (VII) hidroklorida sa 5-klorotiofen-2- karbonil kloridom (IV), naznačen time da se reakcija provodi u otapalu odabranom iz skupine koja sadrži eter, alkohol, keton i vodu ili u njihovoj mješavini uz uporabu anorganske baze.
2. Postupak prema zahtjevu 1, naznačen time da se reakcija provodi u ketonu ili u mješavini ketona i vode kao otapalu.
3. Postupak prema zahtjevu 1 ili 2, naznačen time da se reakcija provodi sa natrijevim hidroksidom, natrijevim karbonatom ili natrijevim bikarbonatom kao anorganskom bazom.
4. Postupak prema bilo kojem od zahtjeva 1 do 3, naznačen time da se reakcija provodi u mješavini aceton/voda kao otapalu uz uporabu natrijevog karbonata kao baze.
5. Postupak prema bilo kojem od zahtjeva 1 do 4, naznačen time da se najprije dovodi vodena otopina natrijevog karbonata, te se reaktanti dodaju kod temperature između 10 i 15°C, te se reakcijska mješavina tada miješa na 50°C.
6. Postupak prema bilo kojem od zahtjeva 1 do 5, naznačen time da je sirovi produkt spoja sa formulom (I) dobiven na ovaj način u slijedećem koraku rekristaliziran iz octene kiseline.
7. Postupak prema bilo kojem od zahtjeva 1 do 6, gdje je aminometiloksazolidinon (VII) hidroklorid dobiven sa uklanjanjem ftalimidne zaštitne skupine iz oksazolidinon metilftalimida (VI) sa metilaminom u etanolu kao otapalu, naznačen time da je aminometiloksazolidinon (VII) izoliran kao hidroklorid u krutom stanju.
8. Postupak prema zahtjevu 7, naznačen time da nakon reakcije oksazolidinonmetilftalimida (VI) sa metilaminom slijedi dodavanje vodene klorovodične kiseline u reakcijsku mješavinu kod temperature između 50 i 60°C dok je pH između 2 i 3.
9. Postupak prema bilo kojem od zahtjeva 7 ili 8, gdje je oksazolidinonmetilftalimid (VI) dobiven sa ciklizacijom hidroksiamino spoja (V) sa ekvivalentom fosgena, naznačen time da se reakcija provodi u toluenu kao otapalu.
10. Postupak prema zahtjevu 9, naznačen time da je oksazolidinonmetilftalimid (VI) izoliran sa filtracijom.
11. Postupak prema bilo kojem od zahtjeva 9 ili 10, gdje je hidroksiamin (V) dobiven sa reakcijom (S)-epoksiftalimida (II) sa anilinomorfolinonom (III) u vodenom etanolu kao otapalu, naznačen time da je omjer etanol/voda 1:2.
12. Postupak prema zahtjevu 11, naznačen time da su zametci kristala reakcijskog produkta (V) dodani u reakcijsku mješavinu nakon što je reakcija trajala od jednog do dva sata.
13. Postupak prema zahtjevu 12, naznačen time da je reakcijska mješavina dva puta grijana pod refluksom prema završetku vremena reakcije, te je svaki puta ponovo naknadno ohladimo na reakcijsku temperaturu od između 55 i 65°C.
HR20110796T 2004-01-15 2011-11-02 Postupak dobivanja HRP20110796T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102004002044A DE102004002044A1 (de) 2004-01-15 2004-01-15 Herstellverfahren
PCT/EP2004/014870 WO2005068456A1 (de) 2004-01-15 2004-12-31 Herstellverfahren

Publications (1)

Publication Number Publication Date
HRP20110796T1 true HRP20110796T1 (hr) 2011-12-31

Family

ID=34716548

Family Applications (1)

Application Number Title Priority Date Filing Date
HR20110796T HRP20110796T1 (hr) 2004-01-15 2011-11-02 Postupak dobivanja

Country Status (33)

Country Link
US (1) US7351823B2 (hr)
EP (1) EP1720866B1 (hr)
JP (2) JP5311742B2 (hr)
KR (1) KR20130004257A (hr)
CN (1) CN1906191B (hr)
AR (1) AR047389A1 (hr)
AT (1) ATE518856T1 (hr)
AU (1) AU2004313694B2 (hr)
BR (1) BRPI0418405B8 (hr)
CA (1) CA2553237C (hr)
CY (1) CY1112565T1 (hr)
DE (1) DE102004002044A1 (hr)
DK (1) DK1720866T3 (hr)
EC (1) ECSP066703A (hr)
ES (1) ES2369140T3 (hr)
GT (1) GT200400277A (hr)
HK (1) HK1103722A1 (hr)
HN (1) HN2005000016A (hr)
HR (1) HRP20110796T1 (hr)
IL (1) IL176767A (hr)
MA (1) MA28290A1 (hr)
MY (1) MY138944A (hr)
NO (1) NO335553B1 (hr)
NZ (1) NZ548506A (hr)
PE (1) PE20050763A1 (hr)
PL (1) PL1720866T3 (hr)
PT (1) PT1720866E (hr)
RU (1) RU2383540C2 (hr)
SI (1) SI1720866T1 (hr)
TW (1) TWI340137B (hr)
UY (1) UY28718A1 (hr)
WO (1) WO2005068456A1 (hr)
ZA (1) ZA200605747B (hr)

Families Citing this family (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19962924A1 (de) 1999-12-24 2001-07-05 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
DE10129725A1 (de) 2001-06-20 2003-01-02 Bayer Ag Kombinationstherapie substituierter Oxazolidinone
DE10300111A1 (de) 2003-01-07 2004-07-15 Bayer Healthcare Ag Verfahren zur Herstellung von 5-Chlor-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophencarboxamid
DE10355461A1 (de) 2003-11-27 2005-06-23 Bayer Healthcare Ag Verfahren zur Herstellung einer festen, oral applizierbaren pharmazeutischen Zusammensetzung
DE102004062475A1 (de) * 2004-12-24 2006-07-06 Bayer Healthcare Ag Feste, oral applizierbare pharmazeutische Darreichungsformen mit modifizierter Freisetzung
EP1685841A1 (en) 2005-01-31 2006-08-02 Bayer Health Care Aktiengesellschaft Prevention and treatment of thromboembolic disorders
DE102005045518A1 (de) 2005-09-23 2007-03-29 Bayer Healthcare Ag 2-Aminoethoxyessigsäure-Derivate und ihre Verwendung
DE102005047564A1 (de) * 2005-10-04 2007-05-31 Bayer Healthcare Ag Amorphe Form von 5-Chlor-N-({(5S)2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl)-methyl)-2-thiophencarboxamid
DE102005047561A1 (de) 2005-10-04 2007-04-05 Bayer Healthcare Ag Feste, oral applizierbare pharmazeutische Darreichungsformen mit schneller Wirkstofffreisetzung
DE102005047558A1 (de) * 2005-10-04 2008-02-07 Bayer Healthcare Ag Kombinationstherapie substituierter Oxazolidinone zur Prophylaxe und Behandlung von cerebralen Durchblutungsstörungen
PL1934208T3 (pl) * 2005-10-04 2011-09-30 Bayer Ip Gmbh Nowa polimorficzna postać 5-chloro-N-({ (5S)-2-okso-3-[4-( 3-okso-4-morfolinylo)-fenylo]-1,3-oksazolidyn-5-ylo}-metylo)-2-tiofenokarboksamidu
DE102006007146A1 (de) 2006-02-16 2007-08-23 Bayer Healthcare Ag Aminoacyl-Prodrugs
DE102006039589A1 (de) * 2006-08-24 2008-03-06 Bayer Healthcare Ag Aminoacyl-Prodrugs II
DE102006051625A1 (de) * 2006-11-02 2008-05-08 Bayer Materialscience Ag Kombinationstherapie substituierter Oxazolidinone
DE102007028319A1 (de) * 2007-06-20 2008-12-24 Bayer Healthcare Ag Substituierte Oxazolidinone und ihre Verwendung
DE102007028407A1 (de) * 2007-06-20 2008-12-24 Bayer Healthcare Ag Substituierte Oxazolidinone und ihre Verwendung
WO2009018807A1 (de) * 2007-08-06 2009-02-12 Schebo Biotech Ag Oxazolidinone als faktor xa- inhibitoren, verfahren zu ihrer herstellung und ihre verwendung in der therapie
US8706950B2 (en) 2008-03-01 2014-04-22 Kabushiki Kaisha Toshiba Memory system
DE102008028071A1 (de) * 2008-06-12 2009-12-17 Bayer Schering Pharma Aktiengesellschaft Neue Cokristall-Verbindung von Rivaroxaban und Malonsäure
US20100168111A1 (en) * 2008-12-31 2010-07-01 Apotex Pharmachem Inc. Polymorphic form of 5 chloro n {[(5s) 2 oxo 3 [4 (3 oxomorpholin 4 yl)phenyl]oxa-zolidin 5 yl]-methyl}thiophene 2 carboxamide
US8435989B2 (en) * 2009-04-28 2013-05-07 Apotex Pharmachem Inc. Processes for the preparation of rivaroxaban and intermediates thereof
US7816355B1 (en) * 2009-04-28 2010-10-19 Apotex Pharmachem Inc Processes for the preparation of rivaroxaban and intermediates thereof
US8309547B2 (en) * 2009-04-28 2012-11-13 Apotex Pharmachem Inc. Processes for the preparation of rivaroxaban and intermediates thereof
WO2011012321A1 (en) 2009-07-31 2011-02-03 Krka, D.D., Novo Mesto Processes for crystallization of rivaroxaban
CN102822167A (zh) * 2010-01-04 2012-12-12 埃南蒂亚有限公司 用于制备利伐沙班的方法及其中间体
DE102010028362A1 (de) 2010-04-29 2011-11-03 Bayer Schering Pharma Aktiengesellschaft Herstellverfahren
EP2388260A1 (de) * 2010-05-21 2011-11-23 Archimica GmbH Herstellungsverfahren für einen Inhibitor eines Blutgerinnungsfaktors
CN107021932A (zh) * 2010-06-29 2017-08-08 欧美嘉股份有限公司 制备5‑左旋‑氨甲基‑3‑芳基‑2‑恶唑烷酮类的方法
EP2404920A1 (en) 2010-07-06 2012-01-11 Sandoz AG Crystalline form of Rivaroxaban dihydrate
US20130253187A1 (en) * 2010-09-14 2013-09-26 Medichem, S.A. Process for Determining the Suitability for Distribution of a Batch of Thiophene-2-Carboxamide Derivative
CZ2010714A3 (cs) * 2010-09-30 2012-04-11 Farmak, A. S. Zpusob výroby 2-({(5S)-2-oxo-3-[4-(3-oxo-4-morfolinyl)fenyl]-1,3oxazolidin-5-yl}methyl)-1H-isoindol-1,3(2H)-dionu ve vysoké optické cistote
EP2630143B1 (en) 2010-10-18 2017-11-29 Apotex Pharmachem Inc. Processes for the preparation of rivaroxaban and intermediates thereof
MD4557C1 (ro) * 2011-05-06 2018-10-31 Egis Gyogysszegyar Nyilvanosan Mukodo Reszvenytarsasag Procedeu de obţinere a rivaroxabanului şi un compus intermediar utilizat în acest procedeu
WO2012156983A1 (en) * 2011-05-16 2012-11-22 Symed Labs Limited Processes for the preparation of 5-chloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl) phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide
ES2395304B1 (es) 2011-05-20 2014-01-16 Interquim, S.A. Procedimiento de obtención de una tiofen-2-carboxamida.
CN102250076A (zh) * 2011-05-27 2011-11-23 横店集团家园化工有限公司 一种利伐沙班中间体及利伐沙班的制备方法
CN102827154B (zh) * 2011-06-14 2015-04-22 上海科胜药物研发有限公司 一种合成利伐沙班中间体4-{4-[(5s)-5-(氨基甲基)-2-氧代-1,3-恶唑烷-3-基]苯基}吗啉-3-酮的方法
EP2753619A2 (en) 2011-09-08 2014-07-16 Cadila Healthcare Limited Processes and intermediates for preparing rivaroxaban
WO2013053739A1 (en) 2011-10-10 2013-04-18 Laboratorios Lesvi, S. L. Process for preparing factor xa inhibitors
WO2013121436A2 (en) * 2012-02-06 2013-08-22 Megafine Pharma (P) Ltd A process for preparation of rivaroxaban and intermediates thereof
CZ2012114A3 (cs) * 2012-02-17 2013-02-20 Zentiva, K.S. Zpusob prípravy rivaroxabanu zalozený na úspore 1,1´ -karbonyldiimidazolu
CN103288814B (zh) 2012-02-24 2016-07-06 国药集团国瑞药业有限公司 一种利伐沙班中间体的制备方法
CN102659756A (zh) * 2012-04-01 2012-09-12 南京哈柏医药科技有限公司 5-氯-2-酰氯噻吩的合成方法
US9562040B2 (en) 2012-04-06 2017-02-07 Indiana University Research And Technology Corporation Processes for preparing Rivaroxaban
ES2871811T3 (es) 2012-05-02 2021-11-02 Symed Labs Ltd Proceso mejorado para preparar rivaroxabán utilizando intermedios novedosos
CN102757424B (zh) * 2012-07-09 2014-10-15 云南大学 2-苄基取代苯并呋喃—咪唑盐类化合物及其制备方法
CN102746288B (zh) * 2012-07-24 2015-04-08 常州制药厂有限公司 一种抗凝血药及其关键中间体的制备方法
WO2014020458A1 (en) * 2012-08-01 2014-02-06 Alembic Pharmaceuticals Limited Improved process for preparation of rivaroxaban
CN102786516B (zh) * 2012-08-21 2014-10-01 湖南师范大学 一种利伐沙班的合成方法
CN103833724A (zh) * 2012-11-20 2014-06-04 上海医药工业研究院 一种5-氯噻吩-2-甲酰氯的制备方法
CN103864772A (zh) * 2012-12-13 2014-06-18 北京京卫信康医药科技发展有限公司 一种利伐沙班及其中间体的制备方法
CN103864771A (zh) * 2012-12-13 2014-06-18 北京京卫信康医药科技发展有限公司 一种利伐沙班的制备方法
WO2014096214A1 (en) * 2012-12-21 2014-06-26 Farma Grs, D.O.O. A process for preparation of rivaroxaban
HUE032850T2 (en) 2012-12-26 2017-11-28 Wanbury Ltd Rivaroxaban intermediate and its preparation
EP2897619A4 (en) 2012-12-26 2016-08-17 Wanbury Ltd ALDEHYDE DERIVATIVE FROM SUBSTITUTED OXAZOLIDINONES
US9663505B2 (en) 2013-03-25 2017-05-30 Glenmark Pharmaceuticals Limited Process for the preparation of rivaroxaban
CN104109158A (zh) * 2013-04-16 2014-10-22 上海医药工业研究院 一种纯化利伐沙班的方法
CN103275061A (zh) * 2013-06-04 2013-09-04 上海同昌生物医药科技有限公司 一种生产5-氯噻吩-2-羧酸的方法
CN103351385A (zh) * 2013-06-28 2013-10-16 浙江燎原药业有限公司 一种利伐沙班中间体的制备方法
CN103709116B (zh) * 2013-12-10 2015-09-23 四川大学 一种4-(4-烷氧羰氨基)苯基-3-吗啉酮的制备方法
CN103724336B (zh) * 2013-12-24 2015-10-21 悦康药业集团有限公司 一种新型抗凝血药物的合成方法
IN2014MU00072A (hr) 2014-01-08 2015-08-21 Wockhardt Ltd
WO2015111076A2 (en) 2014-01-23 2015-07-30 Symed Labs Limited Improved processes for the preparation of highly pure rivaroxaban crystal modification i
CN105085370B (zh) * 2014-04-22 2017-04-12 北大方正集团有限公司 (s)‑1‑卤代‑2‑[2‑(1,3‑二氧异吲哚)基]乙基氯甲酸酯及其制备方法
WO2015188787A1 (en) * 2014-06-14 2015-12-17 Sunshine Lake Pharma Co., Ltd. Method for preparing oxazolidinone compound and intermediates thereof
CN104086539A (zh) * 2014-07-17 2014-10-08 天津炜捷制药有限公司 一种利伐沙班的制备方法
CN104211693B (zh) * 2014-08-07 2017-02-22 成都百裕制药股份有限公司 一种利伐沙班晶型及其制备方法与用途
CN104211694A (zh) * 2014-08-14 2014-12-17 广东东阳光药业有限公司 一种改进的制备Xa因子抑制剂的方法
US20170267669A1 (en) * 2014-08-25 2017-09-21 Cipla Limited Process for the Preparation of Rivaroxaban
EA034656B1 (ru) 2014-10-22 2020-03-03 Закляды Фармацеутычне Польфарма С.А Способ получения полиморфа ривароксабана
CN104807934B (zh) * 2015-04-30 2017-01-18 成都百裕制药股份有限公司 异吲哚二酮类化合物的正相高效液相色谱检测方法
CN105130976A (zh) * 2015-08-26 2015-12-09 浙江车头制药股份有限公司 一种利伐沙班中间体的合成方法
CN105440028B (zh) * 2015-12-07 2018-03-13 石家庄康贺威药业有限公司 一种利伐沙班化合物及其制备方法
CN106008490B (zh) * 2016-01-11 2019-01-04 南京生命能科技开发有限公司 一种利伐沙班的新晶体及其制备方法
CN106977507A (zh) * 2017-04-21 2017-07-25 上海华源医药科技发展有限公司 一种利伐沙班的制备方法
CN109553611A (zh) * 2017-09-23 2019-04-02 齐鲁制药有限公司 利伐沙班中间体的制备方法和用途
JP7205529B2 (ja) * 2018-02-26 2023-01-17 住友化学株式会社 オキサゾリジノン化合物の製造方法
JP7339754B2 (ja) * 2019-03-27 2023-09-06 ダイト株式会社 中間体の製造方法
CN112521380A (zh) * 2020-12-14 2021-03-19 哈尔滨珍宝制药有限公司 一种利伐沙班中间体a的合成方法及其在制备利伐沙班中的应用
BR112023024807A2 (pt) * 2021-05-28 2024-02-15 Merck Sharp & Dohme Llc Síntese de inibidor de btk e intermediários do mesmo
EP4201933A1 (en) 2021-12-23 2023-06-28 Zaklady Farmaceutyczne Polpharma S.A. Crystallisation process for rivaroxaban

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19962924A1 (de) * 1999-12-24 2001-07-05 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
DE10129725A1 (de) * 2001-06-20 2003-01-02 Bayer Ag Kombinationstherapie substituierter Oxazolidinone
DE10300111A1 (de) * 2003-01-07 2004-07-15 Bayer Healthcare Ag Verfahren zur Herstellung von 5-Chlor-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophencarboxamid

Also Published As

Publication number Publication date
CN1906191B (zh) 2010-05-26
ZA200605747B (en) 2007-10-31
DK1720866T3 (da) 2011-11-21
JP5311742B2 (ja) 2013-10-09
CA2553237A1 (en) 2005-07-28
ECSP066703A (es) 2006-10-31
PL1720866T3 (pl) 2012-01-31
JP2007517816A (ja) 2007-07-05
HK1103722A1 (en) 2007-12-28
SI1720866T1 (sl) 2012-01-31
UY28718A1 (es) 2005-08-31
NZ548506A (en) 2009-06-26
IL176767A (en) 2011-04-28
DE102004002044A1 (de) 2005-08-04
MY138944A (en) 2009-08-28
BRPI0418405A (pt) 2007-05-15
KR20130004257A (ko) 2013-01-09
IL176767A0 (en) 2006-10-31
CA2553237C (en) 2012-04-17
US20050182055A1 (en) 2005-08-18
HN2005000016A (es) 2009-06-01
TW200604195A (en) 2006-02-01
JP2012097106A (ja) 2012-05-24
US7351823B2 (en) 2008-04-01
BRPI0418405B1 (pt) 2018-03-13
CN1906191A (zh) 2007-01-31
BRPI0418405B8 (pt) 2021-05-25
ES2369140T3 (es) 2011-11-25
NO20063677L (no) 2006-10-11
NO335553B1 (no) 2014-12-29
PT1720866E (pt) 2011-10-12
GT200400277A (es) 2005-08-18
AU2004313694B2 (en) 2011-06-02
CY1112565T1 (el) 2016-02-10
EP1720866A1 (de) 2006-11-15
PE20050763A1 (es) 2005-12-02
WO2005068456A1 (de) 2005-07-28
AU2004313694A1 (en) 2005-07-28
RU2383540C2 (ru) 2010-03-10
ATE518856T1 (de) 2011-08-15
AR047389A1 (es) 2006-01-18
TWI340137B (en) 2011-04-11
MA28290A1 (fr) 2006-11-01
EP1720866B1 (de) 2011-08-03
RU2006129341A (ru) 2008-02-20

Similar Documents

Publication Publication Date Title
HRP20110796T1 (hr) Postupak dobivanja
AU717699B2 (en) Chemical compounds
JP4790969B2 (ja) ペルオキシソーム増殖剤応答性受容体δの活性化剤
JP4226005B2 (ja) Ｐｐａｒ活性化化合物及びこれを含有する医薬組成物
BRPI0213243B1 (pt) composto heterocíclico aromático contendo um anel oxazol, tiazol ou imidazol, ou um sal farmaceuticamente aceitável do mesmo, e, composição farmacêutica
KR20140128886A (ko) 선택적 히스톤 탈아세틸화 효소 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
JP2012510515A (ja) ジアシルグリセロールアシルトランスフェラーゼの阻害剤
BRPI0609656A2 (pt) piperidinas substituìdas
CA2538906A1 (en) Process for preparing 4-(4-aminophenyl)-3-morpholinone
JP2012512252A (ja) ジアシルグリセロールアシルトランスフェラーゼの阻害剤
JPWO2002046154A1 (ja) ペルオキシソーム増殖剤応答性受容体δの活性化剤
NO330171B1 (no) Kirale oksazol-arylpropionsyrederivater, fremgangsmate for fremstilling av slike, farmasoytisk preparat inneholdende slike, slike forbindelser for anvendelse som terapeutisk aktive substanser samt slike forbindelser for behandling og/eller forbygging av sykdom
AU2010362639A1 (en) Processes for the preparation of Rivaroxaban and intermediates thereof
KR20130087283A (ko) 인돌 및 인다졸 유도체를 유효성분으로 포함하는 암 전이 억제용 조성물
US20140114066A1 (en) Novel method for synthesizing rivaroxaban intermediate, 4-morpholin-3-one
CZ301464B6 (cs) Piperazinové a piperidinové slouceniny, zpusob jejich prípravy a farmaceutické prostredky, které je obsahují
AU2012378913A1 (en) Improved process for preparing rivaroxaban using novel intermediates
KR20010076389A (ko) 벤젠술폰아미드 화합물, 이의 제조 방법 및 이를 함유하는약제 조성물
NO20070972L (no) Benzyloksyderivater som MAOB-inhibitorer
EP3186246A1 (en) Process for the preparation of rivaroxaban
CA2100376A1 (en) Alkylenediamine derivatives
Siddaraj et al. A novel and expeditious synthesis of oxazolidinone drugs linezolid and eperezolid
CA2884433A1 (en) [3-heteroaryl-2-trifluoromethyl-propyl]-piperidin-1 -yle or -morpholin-4-yle compounds as trpa1 antagonists for the treatment of respiratory diseases
TH79777A (th) กระบวนการสำหรับเตรียม 5-คลอโร-n-({(5s)-2-ออกโซ-3-[4-(3-ออกโซ-4-มอร์โฟลินิล)ฟีนิล]-1,3-ออกซาโซลิดีน-5-อิล}เมธิล)-2-ไธโอฟีนคาร์บอกซาไมด์
TH76945B (th) กระบวนการสำหรับเตรียม 5-คลอโร-n-({(5s)-2-ออกโซ-3-[4-(3-ออกโซ-4-มอร์โฟลินิล)ฟีนิล]-1,3-ออกซาโซลิดีน-5-อิล}เมธิล)-2-ไธโอฟีนคาร์บอกซาไมด์