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AR039625A1 - Proceso para la preparacion de 5-((2(r)--(1(r)- (3,5-bis (trifluormetil) fenil)etoxi-3 (s) - (4-fluorfenil) -4-morfolinil) metil) -1,2-dihidro-3h-1,2,4-triazol-3-ona - Google Patents

Proceso para la preparacion de 5-((2(r)--(1(r)- (3,5-bis (trifluormetil) fenil)etoxi-3 (s) - (4-fluorfenil) -4-morfolinil) metil) -1,2-dihidro-3h-1,2,4-triazol-3-ona

Info

Publication number
AR039625A1
AR039625A1 ARP030101248A ARP030101248A AR039625A1 AR 039625 A1 AR039625 A1 AR 039625A1 AR P030101248 A ARP030101248 A AR P030101248A AR P030101248 A ARP030101248 A AR P030101248A AR 039625 A1 AR039625 A1 AR 039625A1
Authority
AR
Argentina
Prior art keywords
compound
triazol
bis
phenyl
methyl
Prior art date
Application number
ARP030101248A
Other languages
English (en)
Original Assignee
Merck & Co Inc
Merck Sharp & Dohme
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, Merck Sharp & Dohme filed Critical Merck & Co Inc
Publication of AR039625A1 publication Critical patent/AR039625A1/es

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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

La presente invención se refiere a un novedoso proceso para la preparación del compuesto 5-[[2(R)-[1(R)-[3,5-bis(trifluormetil)fenil]etoxi]-3(s)-(4-fluorfenil)-4-morfolinil]metil]-1,2-dihidro-3H-1,2,4-triazol-3-ona. Este compuesto es útil como antagonista del receptor de la sustancia P (neuroquina-1). En particular, el compuesto es útil por ejemplo en el tratamiento de trastornos psiquiátricos, enfermedades inflamatorias y emesis. Reivindicación 1: un proceso para preparar un compuesto de la fórmula (1), que comprende: ciclizar un compuesto de la fórmula (4), a una temperatura de 140-150°C a efectos de producir el compuesto de la fórmula (1).
ARP030101248A 2002-04-18 2003-04-09 Proceso para la preparacion de 5-((2(r)--(1(r)- (3,5-bis (trifluormetil) fenil)etoxi-3 (s) - (4-fluorfenil) -4-morfolinil) metil) -1,2-dihidro-3h-1,2,4-triazol-3-ona AR039625A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US37373402P 2002-04-18 2002-04-18

Publications (1)

Publication Number Publication Date
AR039625A1 true AR039625A1 (es) 2005-03-02

Family

ID=29251070

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030101248A AR039625A1 (es) 2002-04-18 2003-04-09 Proceso para la preparacion de 5-((2(r)--(1(r)- (3,5-bis (trifluormetil) fenil)etoxi-3 (s) - (4-fluorfenil) -4-morfolinil) metil) -1,2-dihidro-3h-1,2,4-triazol-3-ona

Country Status (21)

Country Link
US (1) US7847095B2 (es)
EP (1) EP1499611B1 (es)
JP (1) JP4271586B2 (es)
KR (1) KR100982901B1 (es)
CN (1) CN1293077C (es)
AR (1) AR039625A1 (es)
AU (1) AU2003228578B2 (es)
BR (1) BR0309277A (es)
CA (1) CA2482466C (es)
EG (1) EG24127A (es)
HR (1) HRP20040974A2 (es)
IL (1) IL164586A (es)
MX (1) MXPA04010182A (es)
NO (1) NO330362B1 (es)
NZ (1) NZ535883A (es)
PL (1) PL217076B1 (es)
RU (1) RU2326879C2 (es)
TW (1) TWI341313B (es)
UA (1) UA84399C2 (es)
WO (1) WO2003089429A1 (es)
ZA (1) ZA200408193B (es)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE0400850D0 (sv) * 2004-03-30 2004-03-31 Astrazeneca Ab Novel Compounds
EP2266980A1 (en) 2005-10-05 2010-12-29 Ranbaxy Laboratories Limited Polymorphic form of aprepitant intermediate
US8133994B2 (en) 2005-10-06 2012-03-13 Dr. Reddy's Laboratories Ltd. Preparation of aprepitant
KR20080089659A (ko) 2006-02-03 2008-10-07 그렌마크 파머수티칼스 엘티디. 아프레피탄트의 비정질 및 결정 형태 및 그것의 제조 방법
US20090149462A1 (en) * 2006-08-28 2009-06-11 Hetero Drugs Limited Process for purification of aprepitant
CN102939285B (zh) * 2010-05-24 2014-12-24 成都地奥制药集团有限公司 5-[[2(r)-[1(r)-[3,5-双(三氟甲基)苯基]乙氧基]-3(s)-4-(氟苯基)-4-吗啉基]甲基]-1,2-二氢-3h-1,2,4-三唑-3-酮的制备方法
HUP1000325A2 (en) * 2010-06-18 2012-01-30 Druggability Technologies Ip Holdco Jersey Ltd Nanostructured aprepitant compositions and process for their preparation
WO2012146692A1 (en) 2011-04-29 2012-11-01 Sandoz Ag Novel intermediates for the preparation of highly pure aprepitant or fosaprepitant
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
WO2013124823A1 (en) * 2012-02-23 2013-08-29 Piramal Enterprises Limited An improved process for the preparation of aprepitant
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
ITMI20130273A1 (it) * 2013-02-26 2014-08-27 Olon Spa Procedimento per la preparazione di aprepitant
CN103288813A (zh) * 2013-06-04 2013-09-11 四川百利药业有限责任公司 一种阿瑞匹坦的制备方法
CN107954998B (zh) * 2016-10-14 2022-08-12 江苏豪森药业集团有限公司 福沙匹坦中间体的制备方法
CN106967057A (zh) * 2017-06-01 2017-07-21 四川制药制剂有限公司 一种阿瑞匹坦高效制备工艺

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5637699A (en) 1992-06-29 1997-06-10 Merck & Co., Inc. Process for preparing morpholine tachykinin receptor antagonists
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
TW385308B (en) * 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
GB9513972D0 (en) * 1995-07-08 1995-09-06 Merck Sharp & Dohme Pharmaceutical compositions
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

Also Published As

Publication number Publication date
EP1499611A1 (en) 2005-01-26
IL164586A (en) 2010-11-30
PL217076B1 (pl) 2014-06-30
TW200400189A (en) 2004-01-01
UA84399C2 (en) 2008-10-27
AU2003228578B2 (en) 2009-07-30
MXPA04010182A (es) 2005-02-03
EP1499611A4 (en) 2006-05-03
BR0309277A (pt) 2005-02-22
ZA200408193B (en) 2006-06-28
IL164586A0 (en) 2005-12-18
HRP20040974A2 (en) 2005-06-30
RU2004133678A (ru) 2005-05-27
PL373348A1 (en) 2005-08-22
TWI341313B (en) 2011-05-01
CN1646525A (zh) 2005-07-27
CA2482466C (en) 2012-11-20
WO2003089429A1 (en) 2003-10-30
CN1293077C (zh) 2007-01-03
KR100982901B1 (ko) 2010-09-20
AU2003228578A1 (en) 2003-11-03
NO330362B1 (no) 2011-04-04
NZ535883A (en) 2007-12-21
RU2326879C2 (ru) 2008-06-20
KR20050007299A (ko) 2005-01-17
EP1499611B1 (en) 2015-02-11
US7847095B2 (en) 2010-12-07
JP4271586B2 (ja) 2009-06-03
EG24127A (en) 2008-07-08
CA2482466A1 (en) 2003-10-30
JP2005529881A (ja) 2005-10-06
NO20045001L (no) 2004-11-17
US20050215786A1 (en) 2005-09-29

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