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WO2009116081A3 - 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
WO2009116081A3
WO2009116081A3 PCT/IN2009/000134 IN2009000134W WO2009116081A3 WO 2009116081 A3 WO2009116081 A3 WO 2009116081A3 IN 2009000134 W IN2009000134 W IN 2009000134W WO 2009116081 A3 WO2009116081 A3 WO 2009116081A3
Authority
WO
WIPO (PCT)
Prior art keywords
aprepitant
preparation
improved process
intermediates
compound
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/IN2009/000134
Other languages
French (fr)
Other versions
WO2009116081A2 (en
Inventor
Manne Satyanarayana Reddy
Sajja Eswaraiah
Mummadi Venkatesh
Mummadi Venkazesh
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.)
MSN Laboratories Pvt Ltd
Original Assignee
MSN Laboratories Pvt 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 MSN Laboratories Pvt Ltd filed Critical MSN Laboratories Pvt Ltd
Publication of WO2009116081A2 publication Critical patent/WO2009116081A2/en
Anticipated expiration legal-status Critical
Publication of WO2009116081A3 publication Critical patent/WO2009116081A3/en
Ceased legal-status Critical Current

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
    • C07D413/02—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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention relates to an improved process for the preparation of aprepitant compound of formula- (I) as well as novel polymorphs of its intermediates.
PCT/IN2009/000134 2008-03-03 2009-03-02 An improved process for the preparation of aprepitant Ceased WO2009116081A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN526CH2008 2008-03-03
IN526/CHE/2008 2008-03-03

Publications (2)

Publication Number Publication Date
WO2009116081A2 WO2009116081A2 (en) 2009-09-24
WO2009116081A3 true WO2009116081A3 (en) 2011-01-06

Family

ID=41091341

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2009/000134 Ceased WO2009116081A2 (en) 2008-03-03 2009-03-02 An improved process for the preparation of aprepitant

Country Status (1)

Country Link
WO (1) WO2009116081A2 (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2013124823A1 (en) * 2012-02-23 2013-08-29 Piramal Enterprises Limited An improved process for the preparation of aprepitant
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
CN111943904B (en) * 2019-05-15 2023-05-05 南京正大天晴制药有限公司 Refining method of key intermediate of neurokinin 1 receptor antagonist
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 (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6096742A (en) * 1997-07-02 2000-08-01 Merck & Co., Inc. Polymorphic form of a tachykinin receptor antagonist
US6395898B1 (en) * 2000-06-09 2002-05-28 Merck & Co. Inc. Trans-glycosidation process for the synthesis of (2R, 2-alpha-R, 3a)-2-[1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-3-(4-fluorophenyl)-1,4-oxazine
US20040214746A1 (en) * 2001-12-10 2004-10-28 Bosch H. William Pharmaceutical composition of a tachykinin receptor antagonist
WO2007039883A2 (en) * 2005-10-05 2007-04-12 Ranbaxy Laboratories Limited Process for preparation of aprepitant
WO2008026216A2 (en) * 2006-08-28 2008-03-06 Hetero Drugs Limited Process for purification of aprepitant

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6096742A (en) * 1997-07-02 2000-08-01 Merck & Co., Inc. Polymorphic form of a tachykinin receptor antagonist
US6395898B1 (en) * 2000-06-09 2002-05-28 Merck & Co. Inc. Trans-glycosidation process for the synthesis of (2R, 2-alpha-R, 3a)-2-[1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-3-(4-fluorophenyl)-1,4-oxazine
US20040214746A1 (en) * 2001-12-10 2004-10-28 Bosch H. William Pharmaceutical composition of a tachykinin receptor antagonist
WO2007039883A2 (en) * 2005-10-05 2007-04-12 Ranbaxy Laboratories Limited Process for preparation of aprepitant
WO2008026216A2 (en) * 2006-08-28 2008-03-06 Hetero Drugs Limited Process for purification of aprepitant

Also Published As

Publication number Publication date
WO2009116081A2 (en) 2009-09-24

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