AU2001266690A1 - Process for the synthesis of (2r, 2-alpha-r)-4-benzyl-2-(1-(3,5-bis(trifluoromethyl)phenyl) ethoxy)-1,4-oxazin-3-one - Google Patents

Process for the synthesis of (2r, 2-alpha-r)-4-benzyl-2-(1-(3,5-bis(trifluoromethyl)phenyl) ethoxy)-1,4-oxazin-3-one

Info

Publication number
AU2001266690A1
AU2001266690A1 AU2001266690A AU6669001A AU2001266690A1 AU 2001266690 A1 AU2001266690 A1 AU 2001266690A1 AU 2001266690 A AU2001266690 A AU 2001266690A AU 6669001 A AU6669001 A AU 6669001A AU 2001266690 A1 AU2001266690 A1 AU 2001266690A1
Authority
AU
Australia
Prior art keywords
oxazin
trifluoromethyl
ethoxy
benzyl
alpha
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.)
Abandoned
Application number
AU2001266690A
Inventor
Karel M. Jos Brands
Joseph F. Payack
Philip J. Pye
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.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
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 Merck and Co Inc filed Critical Merck and Co Inc
Publication of AU2001266690A1 publication Critical patent/AU2001266690A1/en
Abandoned 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
AU2001266690A 2000-06-08 2001-06-04 Process for the synthesis of (2r, 2-alpha-r)-4-benzyl-2-(1-(3,5-bis(trifluoromethyl)phenyl) ethoxy)-1,4-oxazin-3-one Abandoned AU2001266690A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US21025500P 2000-06-08 2000-06-08
US60210255 2000-06-08
PCT/US2001/018039 WO2001094323A1 (en) 2000-06-08 2001-06-04 Process for the synthesis of (2r, 2-alpha-r)-4-benzyl-2-[1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-1,4-oxazin-3-one

Publications (1)

Publication Number Publication Date
AU2001266690A1 true AU2001266690A1 (en) 2001-12-17

Family

ID=22782181

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2001266690A Abandoned AU2001266690A1 (en) 2000-06-08 2001-06-04 Process for the synthesis of (2r, 2-alpha-r)-4-benzyl-2-(1-(3,5-bis(trifluoromethyl)phenyl) ethoxy)-1,4-oxazin-3-one

Country Status (4)

Country Link
US (1) US6469164B2 (en)
EP (1) EP1292583A4 (en)
AU (1) AU2001266690A1 (en)
WO (1) WO2001094323A1 (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA76810C2 (en) 2001-12-10 2006-09-15 Мерк Енд Ко., Інк. Pharmaceutical compositions of tachikinine receptor antagonist in form of nanoparticles
WO2008080822A1 (en) * 2006-12-29 2008-07-10 F. Hoffmann-La Roche Ag Epimerization methodologies for recovering stereo isomers in high yield and purity
WO2012146692A1 (en) 2011-04-29 2012-11-01 Sandoz Ag Novel intermediates for the preparation of highly pure aprepitant or fosaprepitant
CN103012305B (en) * 2011-09-23 2016-08-17 江苏豪森药业集团有限公司 A kind of preparation method of fosaprepitant intermediate
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
CN102675240B (en) * 2012-04-13 2015-01-14 浙江海正药业股份有限公司 4-substitute-2-hydroxy morpholine-3-ketone and preparation method thereof
CN104327009B (en) * 2014-09-24 2016-07-20 山东省生物医药科学院 A kind of process for purification of Aprepitant key intermediate
CN104447607B (en) * 2014-12-12 2017-02-22 瑞阳制药有限公司 preparation method of Aprepitant intermediate
CN104557760A (en) * 2015-01-28 2015-04-29 武汉励合生物医药科技有限公司 Preparation method of aprepitant intermediate
CN109694360A (en) * 2018-12-28 2019-04-30 凯瑞斯德生化(苏州)有限公司 A kind of preparation method of Aprepitant intermediate
CN112500363A (en) * 2020-12-23 2021-03-16 中山奕安泰医药科技有限公司 Refining method of aprepitant intermediate

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000015621A1 (en) * 1998-09-11 2000-03-23 Merck & Co., Inc. Process for the synthesis of n-benzyl-3-(4-fluorophenyl)-1,4-oxazin-2-one
WO2000026214A1 (en) * 1998-10-30 2000-05-11 Merck & Co., Inc. Linear process for the preparation of a morpholine compound
AR030284A1 (en) * 2000-06-08 2003-08-20 Merck & Co Inc PROCESS FOR THE SYNTHESIS OF (2R, 2-ALFA-R, 3A) -2- [1- (3,5-BIS (TRIFLUOROMETIL) PHENYL) ETOXI] -3- (4-FLUOROPHENIL) -1,4-OXAZINE; SUCH COMPOUND AND ITS POLYMORPHIC FORMS

Also Published As

Publication number Publication date
EP1292583A4 (en) 2004-02-25
US20020052493A1 (en) 2002-05-02
US6469164B2 (en) 2002-10-22
WO2001094323A1 (en) 2001-12-13
EP1292583A1 (en) 2003-03-19

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