ATE529162T1 - Verfahren zur herstellung von (3-(2(r)-((1r)-1-(3,5-bis(trifluoromethyl)pheny )ethoxy)-3(s)-(4- fluorophenyl)morpholin-4-yl)methyl)-5-oxo-4,5- dihydro-(1,2,4)-triazol-1-yl)-phosphonsäure - Google Patents

Verfahren zur herstellung von (3-(2(r)-((1r)-1-(3,5-bis(trifluoromethyl)pheny )ethoxy)-3(s)-(4- fluorophenyl)morpholin-4-yl)methyl)-5-oxo-4,5- dihydro-(1,2,4)-triazol-1-yl)-phosphonsäure

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Publication number
ATE529162T1
ATE529162T1 AT05851364T AT05851364T ATE529162T1 AT E529162 T1 ATE529162 T1 AT E529162T1 AT 05851364 T AT05851364 T AT 05851364T AT 05851364 T AT05851364 T AT 05851364T AT E529162 T1 ATE529162 T1 AT E529162T1
Authority
AT
Austria
Prior art keywords
pheny
triazol
fluorophenyl
morpholine
dihydro
Prior art date
Application number
AT05851364T
Other languages
English (en)
Inventor
James Mcnamara
Louis Matty
Jonathan Rosen
Original Assignee
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 Sharp & Dohme filed Critical Merck Sharp & Dohme
Application granted granted Critical
Publication of ATE529162T1 publication Critical patent/ATE529162T1/de

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • 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]

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AT05851364T 2004-11-05 2005-11-03 Verfahren zur herstellung von (3-(2(r)-((1r)-1-(3,5-bis(trifluoromethyl)pheny )ethoxy)-3(s)-(4- fluorophenyl)morpholin-4-yl)methyl)-5-oxo-4,5- dihydro-(1,2,4)-triazol-1-yl)-phosphonsäure ATE529162T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US62520904P 2004-11-05 2004-11-05
PCT/US2005/039946 WO2006060110A2 (en) 2004-11-05 2005-11-03 Process for preparing {3-[2(r)-[(1r)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(s)-(4-fluorophenyl)morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid

Publications (1)

Publication Number Publication Date
ATE529162T1 true ATE529162T1 (de) 2011-11-15

Family

ID=36263958

Family Applications (1)

Application Number Title Priority Date Filing Date
AT05851364T ATE529162T1 (de) 2004-11-05 2005-11-03 Verfahren zur herstellung von (3-(2(r)-((1r)-1-(3,5-bis(trifluoromethyl)pheny )ethoxy)-3(s)-(4- fluorophenyl)morpholin-4-yl)methyl)-5-oxo-4,5- dihydro-(1,2,4)-triazol-1-yl)-phosphonsäure

Country Status (12)

Country Link
US (2) US7807829B2 (de)
EP (1) EP1809379B1 (de)
JP (1) JP4917541B2 (de)
CN (2) CN103130834A (de)
AR (1) AR051475A1 (de)
AT (1) ATE529162T1 (de)
AU (1) AU2005310240B9 (de)
BR (1) BRPI0517989A (de)
CA (1) CA2586114A1 (de)
ES (1) ES2373451T3 (de)
TW (1) TWI358413B (de)
WO (1) WO2006060110A2 (de)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2260029T1 (sl) * 2008-02-26 2015-01-30 Sandoz Ag Priprava morfolinskih derivatov
EP2303901B2 (de) * 2008-07-17 2018-05-09 Glenmark Pharmaceuticals Limited Fosaprepitant-dimeglumin-zwischenproduktintermediate, neutrales fosaprepitant und amorphes fosaprepitant-dimeglumin sowie verfahren zu ihrer herstellung
WO2011045817A2 (en) 2009-10-15 2011-04-21 Sandoz Private Limited Process for the preparation of fosaprepitant, intermediate and pharmaceutical acceptable salt thereof
CN102166199B (zh) * 2011-04-02 2012-11-07 武汉希熙生物科技有限公司 一种注射用福沙吡坦二甲葡胺冻干制剂的制备方法
WO2012146692A1 (en) 2011-04-29 2012-11-01 Sandoz Ag Novel intermediates for the preparation of highly pure aprepitant or fosaprepitant
CN102850398B (zh) * 2011-06-27 2015-06-10 上海医药工业研究院 制备福沙匹坦的方法
CN102977142B (zh) * 2011-09-02 2017-03-29 江苏豪森药业集团有限公司 福沙匹坦二甲葡胺的制备方法
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
CN103183708A (zh) * 2011-12-31 2013-07-03 扬子江药业集团上海海尼药业有限公司 福沙吡坦二甲葡胺的制备方法
CN102558232B (zh) * 2011-12-31 2015-04-08 江苏奥赛康药业股份有限公司 一种福沙吡坦二甲葡胺的制备方法
WO2013168176A2 (en) * 2012-03-30 2013-11-14 Glenmark Generics Limited Process for preparation of fosaprepitant and salt thereof
CN102675369B (zh) * 2012-05-16 2017-07-11 北京华众思康医药技术有限公司 一种制备[3‑[(2r)‑[(1r)‑1‑[3，5‑二(三氟甲基)苯基]乙氧基]‑3(s)‑(4‑氟苯基)吗啉‑4‑基]甲基]‑5‑氧代‑4，5‑二氢‑[1，2，4]‑三唑‑1‑基]膦酸一苄酯的新方法
CN102838634B (zh) * 2012-09-28 2015-05-13 江苏奥赛康药业股份有限公司 一种降低化合物中钯残留的方法及应用这种方法的高纯度福沙匹坦二甲葡胺的制备方法
CN102850399B (zh) * 2012-09-28 2015-03-04 江苏奥赛康药业股份有限公司 一种福沙匹坦二甲葡胺的精制方法
CN103159797A (zh) * 2013-03-29 2013-06-19 山东罗欣药业股份有限公司 福沙吡坦二甲葡胺晶型化合物
CN103204878A (zh) * 2013-03-29 2013-07-17 山东罗欣药业股份有限公司 一种福沙吡坦二甲葡胺的合成方法
CN104098604B (zh) * 2013-04-10 2016-12-28 山东省生物药物研究院 一种制备福沙匹坦二甲葡胺的方法
CN105254668B (zh) * 2013-05-14 2017-10-10 北京百川汇德医药技术开发有限公司 一种福沙匹坦及其可药用盐的制备新方法
IN2013MU03772A (de) * 2013-12-02 2015-07-31 Piramal Entpr Ltd
US9850267B2 (en) 2015-06-03 2017-12-26 Navinta, Llc Crystalline fosaprepitant dicyclohexylamine salt and its preparation
JP7110094B2 (ja) * 2015-11-19 2022-08-01 バイオヘイブン・ファーマシューティカル・ホールディング・カンパニー・リミテッド 医薬化合物のアミンプロドラッグ
WO2017093899A1 (en) 2015-12-01 2017-06-08 Piramal Enterprises Limited A process for preparation of fosaprepitant dimeglumine and an intermediate thereof
CN108948080B (zh) * 2017-05-22 2022-03-04 齐鲁制药有限公司 一种福沙匹坦药用盐的制备方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW385308B (en) * 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
JP2004517045A (ja) * 2000-08-18 2004-06-10 ザ ボード オブ トラスティーズ オブ ザ ユニバーシティ オブ イリノイ 癌およびｈｉｖの治療用ベツリン酸誘導体のプロドラッグ

Also Published As

Publication number Publication date
AU2005310240A1 (en) 2006-06-08
US7915407B2 (en) 2011-03-29
WO2006060110A3 (en) 2006-08-17
TWI358413B (en) 2012-02-21
US20070265442A1 (en) 2007-11-15
AR051475A1 (es) 2007-01-17
CA2586114A1 (en) 2006-06-08
BRPI0517989A (pt) 2008-10-21
EP1809379B1 (de) 2011-10-19
US7807829B2 (en) 2010-10-05
CN101056672A (zh) 2007-10-17
CN103130834A (zh) 2013-06-05
EP1809379A2 (de) 2007-07-25
AU2005310240B9 (en) 2011-10-13
AU2005310240B2 (en) 2011-06-09
TW200631959A (en) 2006-09-16
JP2008518970A (ja) 2008-06-05
ES2373451T3 (es) 2012-02-03
US20100324287A1 (en) 2010-12-23
WO2006060110A2 (en) 2006-06-08
JP4917541B2 (ja) 2012-04-18

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