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WO2009001203A3 - An improved process for the preparation of aprepitant - Google Patents

An improved process for the preparation of aprepitant Download PDF

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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
French (fr)
Other versions
WO2009001203A2 (en
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/en
Publication of WO2009001203A3 publication Critical patent/WO2009001203A3/en
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

The present invention relates to an improved process for the preparation of Aprepitant of formula (I) and its intermediates. More particularly the present invention relates to the preparation of 3-(-S)-(4-fluorophenyl)-4-benzyl-2-morpholinone of Formula (III) or its salts thereof by reacting N-benzyl-(S)-(4-fluorophenyl) glycine of formula (II) with 1,2 dibromoethane in presence of an organic base.
PCT/IB2008/001674 2007-06-27 2008-06-26 An improved process for the preparation of aprepitant Ceased WO2009001203A2 (en)

Applications Claiming Priority (2)

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

Publications (2)

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

Family

ID=40186095

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2008/001674 Ceased WO2009001203A2 (en) 2007-06-27 2008-06-26 An improved process for the preparation of aprepitant

Country Status (1)

Country Link
WO (1) WO2009001203A2 (en)

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 (en) * 2010-05-24 2014-12-24 成都地奥制药集团有限公司 Preparation method of 5-[[2(r)-[1(r)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(s)-4-fluorophenyl-4-morpholinyl]methyl]-1,2-dihydro-3h-1,2,4-triazole-3-one
HUP1000325A2 (en) 2010-06-18 2012-01-30 Druggability Technologies Ip Holdco Jersey Ltd Nanostructured aprepitant compositions and process for their preparation
CN102352389A (en) * 2011-09-29 2012-02-15 重庆邮电大学 Chemical enzyme method for preparing L-para fluobenzene glycine
CZ304770B6 (en) 2012-03-13 2014-10-08 Zentiva, K.S. Process for preparing 3-(((2R,3S)-2-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorfenyl)morpholino)methyl)-1H-1,2,4-triazol-5(4H)-one (aprepitant) in polymorphous form II
CN103694146B (en) * 2013-12-04 2015-10-28 深圳万乐药业有限公司 The preparation method of 2-(the chloro-1-ethylidene of 2-) hydrazides methyl-formiate
CN110746371B (en) * 2019-11-20 2022-07-15 山东鲁抗医药股份有限公司 Intermediate for preparing aprepitant and preparation method and application thereof
CN112939885A (en) * 2021-02-05 2021-06-11 海南鑫开源医药科技有限公司 Preparation method of aprepitant key intermediate

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 (en) * 2005-10-05 2007-04-12 Ranbaxy Laboratories Limited Process for preparation of aprepitant
WO2007044829A2 (en) * 2005-10-06 2007-04-19 Dr. Reddy's Laboratories Ltd. Preparation of 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 (en) * 2005-10-05 2007-04-12 Ranbaxy Laboratories Limited Process for preparation of aprepitant
WO2007044829A2 (en) * 2005-10-06 2007-04-19 Dr. Reddy's Laboratories Ltd. Preparation of aprepitant

Also Published As

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

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