HUP0400491A2 - Eljárás (2R,2-alfa-R,3A)-2-[1-[3,5-bisz(trifluormetil)fenil]-etoxi-3-(4-fluorfenil)-1,4-oxazin előállítására - Google Patents

Eljárás (2R,2-alfa-R,3A)-2-[1-[3,5-bisz(trifluormetil)fenil]-etoxi-3-(4-fluorfenil)-1,4-oxazin előállítására

Info

Publication number
HUP0400491A2
HUP0400491A2 HU0400491A HUP0400491A HUP0400491A2 HU P0400491 A2 HUP0400491 A2 HU P0400491A2 HU 0400491 A HU0400491 A HU 0400491A HU P0400491 A HUP0400491 A HU P0400491A HU P0400491 A2 HUP0400491 A2 HU P0400491A2
Authority
HU
Hungary
Prior art keywords
oxazine
fluorophenyl
trifluoromethyl
ethoxy
alpha
Prior art date
Application number
HU0400491A
Other languages
English (en)
Inventor
Karel M. Jos Brands
Karen M. Conrad
Fuh-Rong Tsay
Matthew M. Zhao
Original Assignee
Merck & 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 & Co., Inc. filed Critical Merck & Co., Inc.
Publication of HUP0400491A2 publication Critical patent/HUP0400491A2/hu

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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

A tatálmány tárgya eljárás (I) képletű (2R,2-alfa-R,3a)-2-[1-[3,5 -bisz(trifluormetil)fenil]etoxi-3-(4-fluorfenil)-1,4-oxazinelőállítására, amely köztitermékként hasznosítható egyes terápiáságensek előállításánál. Közelebbről a találmány tárgya eljárás (2R,2-alfa-R,3a)-2 -[1-[3,5-bisz(trifluormetil)fenil]etoxi-3-(4-fluorfenil)-1,4-oxazin előállítására, amely a P anyag (neurokinin-1) receptorantagonista hatású vegyületek előállításánál köztitermékkénthasznosítható. A találmány értelmében úgy járnak el, hogy a (II)képletű vegyületet valamely (III) általános képletű vegyülettel - aképletben Y jelentése MgCI, MgBr, MgI vagy Li - reagáltatják egy elsőoldószerben, majd hidrogénezést hajtanak végre egy másodikoldószerben. Ó
HU0400491A 2000-06-08 2001-06-04 Eljárás (2R,2-alfa-R,3A)-2-[1-[3,5-bisz(trifluormetil)fenil]-etoxi-3-(4-fluorfenil)-1,4-oxazin előállítására HUP0400491A2 (hu)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US21020300P 2000-06-08 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
HUP0400491A2 true HUP0400491A2 (hu) 2004-06-28

Family

ID=22781976

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0400491A HUP0400491A2 (hu) 2000-06-08 2001-06-04 Eljárás (2R,2-alfa-R,3A)-2-[1-[3,5-bisz(trifluormetil)fenil]-etoxi-3-(4-fluorfenil)-1,4-oxazin előállítására

Country Status (19)

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

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1292583A4 (en) * 2000-06-08 2004-02-25 Merck & Co Inc METHOD FOR PRODUCING (2R, 2-ALPHA-R) -4-BENZYL-2- 1- (3,5-BIS (TRIFLUOROMETHYL) PHENYL) ETHOXY] -1,4-OXAZIN-3-ON
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
CN111665016B (zh) * 2020-06-09 2022-03-08 重庆交通大学 一种河道泡漩结构识别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
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
CA2178219C (en) 1993-12-29 2005-03-22 Raymond Baker 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
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
EP1124826A1 (en) 1998-10-30 2001-08-22 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
WO2000026214A1 (en) 1998-10-30 2000-05-11 Merck & Co., Inc. Linear process for the preparation of a morpholine compound
ATE430144T1 (de) * 1998-12-29 2009-05-15 Pharmacia & Upjohn Co Llc Verfahren zur herstellung von arylethern

Also Published As

Publication number Publication date
HRP20020973A2 (en) 2005-02-28
US20020052494A1 (en) 2002-05-02
SK17082002A3 (sk) 2003-04-01
WO2001094324A1 (en) 2001-12-13
CZ20024013A3 (cs) 2003-03-12
EP1292584A1 (en) 2003-03-19
CN1436178A (zh) 2003-08-13
EA200300002A1 (ru) 2003-04-24
AR030284A1 (es) 2003-08-20
BR0111472A (pt) 2004-01-06
CA2410404A1 (en) 2001-12-13
KR20030007887A (ko) 2003-01-23
JP2003535852A (ja) 2003-12-02
PL359137A1 (en) 2004-08-23
AU2001268170A1 (en) 2001-12-17
MXPA02012101A (es) 2003-04-25
IL152793A0 (en) 2003-06-24
US6600040B2 (en) 2003-07-29
CN1182125C (zh) 2004-12-29
EA004743B1 (ru) 2004-08-26
NZ523389A (en) 2004-08-27

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