AU2001268170A1 - Process for the synthesis of (2r, 2-alpha-r, 3a)-2-(1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3- (4-fluorophenyl)-1,4-oxazine - Google Patents

Process for the synthesis of (2r, 2-alpha-r, 3a)-2-(1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3- (4-fluorophenyl)-1,4-oxazine

Info

Publication number
AU2001268170A1
AU2001268170A1 AU2001268170A AU6817001A AU2001268170A1 AU 2001268170 A1 AU2001268170 A1 AU 2001268170A1 AU 2001268170 A AU2001268170 A AU 2001268170A AU 6817001 A AU6817001 A AU 6817001A AU 2001268170 A1 AU2001268170 A1 AU 2001268170A1
Authority
AU
Australia
Prior art keywords
solvent
bis
palladium
trifluoromethyl
phenyl
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
AU2001268170A
Other languages
English (en)
Inventor
Karel M. Jos Brands
Karen M. Conrad
Fuh-Rong Tsay
Matthew M. Zhao
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 AU2001268170A1 publication Critical patent/AU2001268170A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/321,4-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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
AU2001268170A 2000-06-08 2001-06-04 Process for the synthesis of (2r, 2-alpha-r, 3a)-2-(1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3- (4-fluorophenyl)-1,4-oxazine Abandoned AU2001268170A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US21020300P 2000-06-08 2000-06-08
US60210203 2000-06-08
PCT/US2001/018042 WO2001094324A1 (en) 2000-06-08 2001-06-04 Process for the synthesis of (2r, 2-alpha-r, 3a)-2-[1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-3-(4-fluorophenyl)-1,4-oxazine

Publications (1)

Publication Number Publication Date
AU2001268170A1 true AU2001268170A1 (en) 2001-12-17

Family

ID=22781976

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2001268170A Abandoned AU2001268170A1 (en) 2000-06-08 2001-06-04 Process for the synthesis of (2r, 2-alpha-r, 3a)-2-(1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3- (4-fluorophenyl)-1,4-oxazine

Country Status (19)

Country Link
US (1) US6600040B2 (xx)
EP (1) EP1292584A1 (xx)
JP (1) JP2003535852A (xx)
KR (1) KR20030007887A (xx)
CN (1) CN1182125C (xx)
AR (1) AR030284A1 (xx)
AU (1) AU2001268170A1 (xx)
BR (1) BR0111472A (xx)
CA (1) CA2410404A1 (xx)
CZ (1) CZ20024013A3 (xx)
EA (1) EA004743B1 (xx)
HR (1) HRP20020973A2 (xx)
HU (1) HUP0400491A2 (xx)
IL (1) IL152793A0 (xx)
MX (1) MXPA02012101A (xx)
NZ (1) NZ523389A (xx)
PL (1) PL359137A1 (xx)
SK (1) SK17082002A3 (xx)
WO (1) WO2001094324A1 (xx)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111829749A (zh) * 2020-07-27 2020-10-27 中国空气动力研究与发展中心高速空气动力研究所 一种用于风洞超声速流校大行程单点移测装置及布线方法
CN114235340A (zh) * 2020-06-09 2022-03-25 重庆交通大学 河道泡漩结构跟踪方法及通航预警方法

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001094323A1 (en) * 2000-06-08 2001-12-13 Merck & Co., Inc. Process for the synthesis of (2r, 2-alpha-r)-4-benzyl-2-[1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-1,4-oxazin-3-one
FR2876101B1 (fr) * 2004-10-05 2007-03-02 Sidem Pharma Sa Sa Procede de preparation enantioselective de derives de sulfoxydes
WO2012146692A1 (en) 2011-04-29 2012-11-01 Sandoz Ag Novel intermediates for the preparation of highly pure aprepitant or fosaprepitant
CN103012305B (zh) * 2011-09-23 2016-08-17 江苏豪森药业集团有限公司 一种福沙匹坦中间体的制备方法
CN103030668B (zh) * 2011-10-09 2016-06-15 江苏豪森药业集团有限公司 一种制备福沙匹坦二甲葡胺的方法
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
CN102675240B (zh) 2012-04-13 2015-01-14 浙江海正药业股份有限公司 4-取代基-2-羟基吗啉-3-酮及其制备方法
CN104327009B (zh) * 2014-09-24 2016-07-20 山东省生物医药科学院 一种阿瑞匹坦关键中间体的精制方法
CN104447607B (zh) * 2014-12-12 2017-02-22 瑞阳制药有限公司 阿瑞匹坦中间体的制备方法
CN104557760A (zh) * 2015-01-28 2015-04-29 武汉励合生物医药科技有限公司 阿瑞吡坦中间体的制备方法
CN106397349A (zh) * 2016-08-31 2017-02-15 安徽省润生医药股份有限公司 一种阿瑞吡坦中间体及其制备方法
CN109516964B (zh) * 2017-09-19 2022-05-31 鲁南制药集团股份有限公司 一种阿瑞匹坦中间体的制备方法
CN109694360A (zh) * 2018-12-28 2019-04-30 凯瑞斯德生化(苏州)有限公司 一种阿瑞匹坦中间体的制备方法
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
CN113582982B (zh) * 2021-06-15 2023-06-16 山东罗欣药业集团股份有限公司 一种nk1受体拮抗剂的制备方法

Family Cites Families (9)

* 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
IL111960A (en) * 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
EP0737192B1 (en) 1993-12-29 2001-10-31 Merck Sharp & Dohme Ltd. Substituted morpholine derivatives and their use as therapeutic agents
ZA985765B (en) 1997-07-02 1999-08-04 Merck & Co Inc Polymorphic form of a tachykinin receptor antagonist.
GB9813025D0 (en) 1998-06-16 1998-08-12 Merck Sharp & Dohme Chemical synthesis
CA2342213A1 (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
CA2348526A1 (en) 1998-10-30 2000-05-11 Merck & Co., Inc. Process for the preparation of 2-(r)-(1- (r)-(3,5-bis (trifluoromethyl) phenyl)ethoxy) -4-((5-dimethylaminomethyl) -1,2,3-triazol -4-yl)methyl) -3-(s)-(4- fluorophenyl) morpholine
AU1230000A (en) 1998-10-30 2000-05-22 Merck & Co., Inc. Linear process for the preparation of a morpholine compound
SI1140788T1 (en) * 1998-12-29 2004-08-31 Pharmacia & Upjohn Company Method for the preparation of aryl ethers

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114235340A (zh) * 2020-06-09 2022-03-25 重庆交通大学 河道泡漩结构跟踪方法及通航预警方法
CN114235340B (zh) * 2020-06-09 2023-11-10 重庆交通大学 河道泡漩结构跟踪方法及通航预警方法
CN111829749A (zh) * 2020-07-27 2020-10-27 中国空气动力研究与发展中心高速空气动力研究所 一种用于风洞超声速流校大行程单点移测装置及布线方法

Also Published As

Publication number Publication date
PL359137A1 (en) 2004-08-23
JP2003535852A (ja) 2003-12-02
WO2001094324A1 (en) 2001-12-13
US20020052494A1 (en) 2002-05-02
NZ523389A (en) 2004-08-27
CA2410404A1 (en) 2001-12-13
MXPA02012101A (es) 2003-04-25
IL152793A0 (en) 2003-06-24
CN1182125C (zh) 2004-12-29
EA004743B1 (ru) 2004-08-26
HUP0400491A2 (hu) 2004-06-28
CZ20024013A3 (cs) 2003-03-12
SK17082002A3 (sk) 2003-04-01
CN1436178A (zh) 2003-08-13
EA200300002A1 (ru) 2003-04-24
HRP20020973A2 (en) 2005-02-28
BR0111472A (pt) 2004-01-06
KR20030007887A (ko) 2003-01-23
EP1292584A1 (en) 2003-03-19
AR030284A1 (es) 2003-08-20
US6600040B2 (en) 2003-07-29

Similar Documents

Publication Publication Date Title
US6600040B2 (en) Process for the synthesis of (2R, 2-alpha-R, 3A)-2-[1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-3-(4-fluorophenyl)-1, 4-oxazine
US6469164B2 (en) Process for the synthesis of (2R, 2-alpha-R)-4-benzyl-2-[1-(3,5-bis (trifluoromethyl)phenyl)ethoxy]-1,4-oxazine-3-one
US7847095B2 (en) Process for 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-triazol-3-one
NO180120B (no) Fremgangsmåte ved fremstilling av delmopinol
US6395898B1 (en) 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
KR20010052886A (ko) 모르폴린 유도체의 화학적 합성
US6538134B2 (en) 4-Benzyl-2-hydroxy-1,4-oxazine-3-one and polymorphic forms thereof
JP2002511434A (ja) 2−アリール−l−置換ブタン−2,3−ジオールの不斉合成
US6403793B2 (en) Intramolecular 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
MXPA02000307A (es) Metodo para preparar derivados de 2- (2-arilmorfolin-2-il) etanol y compuestos intermedios.
JP2002275112A (ja) ビナフトール化合物およびその製造法
HU185703B (en) Process for producing conzenzed morpoline derivatives
US6392039B1 (en) Method for preparing (R)-(+)-3 {1-[2-(4-benzoyl-2(3, 4-difluorophenyl)morpholin-2-yl)ethyl]-4-phenylpiperidin-4-yl}-1,1-dimethylurea, its salts solvates and/or hydrates
JPS6120529B2 (xx)
JPH07103098B2 (ja) 1‐置換(s)‐および(r)‐2‐アミノメチルピロリジン類の有効な立体保存的合成およびその中間体
JP3275232B2 (ja) ジヒドロピリジン誘導体の製法
WO2002028834A1 (en) Process for the preparation of aryl-piperidine carbinols and intermediates thereof
EP0915699A4 (en) STEREPSELECTIVE SYNTHESIS OF ENDOTHELIN RECEPTOR ANTAGONISTS
JP2002255926A (ja) 光学活性アリールアルキルアミン化合物の製造法

Legal Events

Date Code Title Description
MK4 Application lapsed section 142(2)(d) - no continuation fee paid for the application