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WO2009001203A3 - Procédé perfectionné pour la préparation d'aprépitant - Google Patents

Procédé perfectionné pour la préparation d'aprépitant Download PDF

Info

Publication number
WO2009001203A3
WO2009001203A3 PCT/IB2008/001674 IB2008001674W WO2009001203A3 WO 2009001203 A3 WO2009001203 A3 WO 2009001203A3 IB 2008001674 W IB2008001674 W IB 2008001674W WO 2009001203 A3 WO2009001203 A3 WO 2009001203A3
Authority
WO
WIPO (PCT)
Prior art keywords
preparation
aprepitant
improved process
formula
fluorophenyl
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/IB2008/001674
Other languages
English (en)
Other versions
WO2009001203A2 (fr
Inventor
Sampath Kumar Upparapalli
Sivadas Anand
Senthilnathan Palanivel
Lakshmi Sivalingam
Loganathan Veluppillai
Siripragada Mahender Rao
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Orchid Pharma Ltd
Original Assignee
Orchid Chemicals and Pharmaceuticals 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 Orchid Chemicals and Pharmaceuticals Ltd filed Critical Orchid Chemicals and Pharmaceuticals Ltd
Priority claimed from IN1376CH2007 external-priority patent/IN2007CH01376A/en
Publication of WO2009001203A2 publication Critical patent/WO2009001203A2/fr
Publication of WO2009001203A3 publication Critical patent/WO2009001203A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
    • 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
    • C07D413/06—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 carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

La présente invention sur un procédé perfectionné pour la préparation d'Aprépitant de formule (I) et de ses intermédiaires. Plus particulièrement, la présente invention porte sur la préparation de la 3-(-S)-(4-fluorophényl)-4-benzyl-2-morpholinone de Formule (III) ou ses sels par réaction de la N-benzyl-(S)-(4-fluorophényl) glycine de formule (II) avec le 1,2-dibromoéthane en présence d'une base organique.
PCT/IB2008/001674 2007-06-27 2008-06-26 Procédé perfectionné pour la préparation d'aprépitant Ceased WO2009001203A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN1376/CHE/2007 2007-06-27
IN1376CH2007 IN2007CH01376A (fr) 2005-02-24 2008-06-26

Publications (2)

Publication Number Publication Date
WO2009001203A2 WO2009001203A2 (fr) 2008-12-31
WO2009001203A3 true WO2009001203A3 (fr) 2009-02-26

Family

ID=40186095

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2008/001674 Ceased WO2009001203A2 (fr) 2007-06-27 2008-06-26 Procédé perfectionné pour la préparation d'aprépitant

Country Status (1)

Country Link
WO (1) WO2009001203A2 (fr)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8816072B2 (en) 2009-06-02 2014-08-26 Ranbaxy Laboratories Limited Process for the preparation of crystalline aprepitant having form I content
CN102939285B (zh) * 2010-05-24 2014-12-24 成都地奥制药集团有限公司 5-[[2(r)-[1(r)-[3,5-双(三氟甲基)苯基]乙氧基]-3(s)-4-(氟苯基)-4-吗啉基]甲基]-1,2-二氢-3h-1,2,4-三唑-3-酮的制备方法
HUP1000325A2 (en) 2010-06-18 2012-01-30 Druggability Technologies Ip Holdco Jersey Ltd Nanostructured aprepitant compositions and process for their preparation
CN102352389A (zh) * 2011-09-29 2012-02-15 重庆邮电大学 一种制备l-对氟苯甘氨酸的化学-酶法
CZ304770B6 (cs) 2012-03-13 2014-10-08 Zentiva, K.S. Způsob výroby 3-(((2R,3S)-2-((R)-1-(3,5-bis(trifluormethyl)fenyl)ethoxy)-3-(4-fluorfenyl)morfolino)methyl)-1H-1,2,4-triazol-5(4H)-onu (Aprepitantu) v polymorfní formě II
CN103694146B (zh) * 2013-12-04 2015-10-28 深圳万乐药业有限公司 2-(2-氯-1-亚乙基)酰肼甲酸甲酯的制备方法
CN110746371B (zh) * 2019-11-20 2022-07-15 山东鲁抗医药股份有限公司 制备阿瑞匹坦的中间体及其制备方法与应用
CN112939885A (zh) * 2021-02-05 2021-06-11 海南鑫开源医药科技有限公司 一种阿瑞吡坦关键中间体的制备方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5719147A (en) * 1992-06-29 1998-02-17 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
GB2341386A (en) * 1998-09-11 2000-03-15 Merck Sharp & Dohme Synthesis of 1,4-oxazin-2-ones
WO2007039883A2 (fr) * 2005-10-05 2007-04-12 Ranbaxy Laboratories Limited Procede permettant de preparer de l'aprepitant
WO2007044829A2 (fr) * 2005-10-06 2007-04-19 Dr. Reddy's Laboratories Ltd. Preparation de l'aprepitant

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5719147A (en) * 1992-06-29 1998-02-17 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
GB2341386A (en) * 1998-09-11 2000-03-15 Merck Sharp & Dohme Synthesis of 1,4-oxazin-2-ones
WO2007039883A2 (fr) * 2005-10-05 2007-04-12 Ranbaxy Laboratories Limited Procede permettant de preparer de l'aprepitant
WO2007044829A2 (fr) * 2005-10-06 2007-04-19 Dr. Reddy's Laboratories Ltd. Preparation de l'aprepitant

Also Published As

Publication number Publication date
WO2009001203A2 (fr) 2008-12-31

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