WO2011045817A3 - Process for the preparation of fosaprepitant - Google Patents

Process for the preparation of fosaprepitant Download PDF

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Publication number
WO2011045817A3
WO2011045817A3 PCT/IN2010/000757 IN2010000757W WO2011045817A3 WO 2011045817 A3 WO2011045817 A3 WO 2011045817A3 IN 2010000757 W IN2010000757 W IN 2010000757W WO 2011045817 A3 WO2011045817 A3 WO 2011045817A3
Authority
WO
WIPO (PCT)
Prior art keywords
fosaprepitant
preparation
manufacture
present
improved process
Prior art date
Application number
PCT/IN2010/000757
Other languages
French (fr)
Other versions
WO2011045817A2 (en
Inventor
Shreerang Joshi
Rashid Khan
Tonmoy Das
Parven Kumar Luthra
Syed Aziz
Original Assignee
Sandoz Ag
Sandoz Private Limited
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 Sandoz Ag, Sandoz Private Limited filed Critical Sandoz Ag
Publication of WO2011045817A2 publication Critical patent/WO2011045817A2/en
Publication of WO2011045817A3 publication Critical patent/WO2011045817A3/en

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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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

The present invention relates to an improved process for the manufacture of phosphorylated Aprepitant and intermediate thereof. The present invention further relates to an improved process for the manufacture of Fosaprepitant dimeglumine from the said intermediate.
PCT/IN2010/000757 2009-10-15 2010-10-13 Process for the preparation of fosaprepitant, intermediate and pharmaceutical acceptable salt thereof WO2011045817A2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
IN1255/KOL/2009 2009-10-15
IN1255KO2009 2009-10-15
IN2414/MUM/2010 2010-08-30
IN2414MU2010 2010-08-30

Publications (2)

Publication Number Publication Date
WO2011045817A2 WO2011045817A2 (en) 2011-04-21
WO2011045817A3 true WO2011045817A3 (en) 2011-07-14

Family

ID=43608175

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2010/000757 WO2011045817A2 (en) 2009-10-15 2010-10-13 Process for the preparation of fosaprepitant, intermediate and pharmaceutical acceptable salt thereof

Country Status (1)

Country Link
WO (1) WO2011045817A2 (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN2011CH01927A (en) 2011-06-03 2015-10-02 Hetero Research Foundation
CN102977142B (en) * 2011-09-02 2017-03-29 江苏豪森药业集团有限公司 The preparation method of fosaprepitant dimeglumine
CN103030668B (en) * 2011-10-09 2016-06-15 江苏豪森药业集团有限公司 A kind of method preparing fosaprepitant
CN102558232B (en) * 2011-12-31 2015-04-08 江苏奥赛康药业股份有限公司 Preparation method of fosaprepitant dimeglumine
CN103183708A (en) * 2011-12-31 2013-07-03 扬子江药业集团上海海尼药业有限公司 Preparation method for fosaprepitant dimeglumine
WO2013168176A2 (en) * 2012-03-30 2013-11-14 Glenmark Generics Limited Process for preparation of fosaprepitant and salt thereof
CN102675369B (en) * 2012-05-16 2017-07-11 北京华众思康医药技术有限公司 One kind prepares [3 [(2R) [(1R) 1 [3,5 two (trifluoromethyl) phenyl] ethyoxyl] 3 (S) (4 fluorophenyl) morpholines 4 base] methyl] 5 oxos 4,5 dihydros [1,2,4] base of triazole 1] benzyl ester of phosphonic acids one new method
CN104650141A (en) * 2013-11-22 2015-05-27 上海汇伦生命科技有限公司 Refining method of fosaprepitant dimeglumine
CN107353303B (en) 2016-05-09 2020-09-01 上海奥博生物医药技术有限公司 Preparation method of fosaprepitant phosphate intermediate
CN109608498A (en) * 2018-12-25 2019-04-12 四川制药制剂有限公司 A kind of Fosaprepitant supercritical reaction preparation method
CN111662329B (en) * 2020-06-22 2021-03-30 连云港贵科药业有限公司 Synthesis method of fosaprepitant meglumine
CN113583044B (en) * 2021-06-15 2023-11-14 山东罗欣药业集团股份有限公司 Preparation method of medicine for preventing chemotherapy-related nausea and vomiting

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995023798A1 (en) * 1994-03-04 1995-09-08 Merck & Co., Inc. Prodrugs of morpholine tachykinin receptor antagonists
WO2006060110A2 (en) * 2004-11-05 2006-06-08 Merck & Co., Inc. 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
WO2010018595A2 (en) * 2008-07-17 2010-02-18 Glenmark Generics Limited Fosaprepitant dimeglumine intermediate, neutral fosaprepitant, and amorphous fosaprepitant dimeglumine and processes for their preparations

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995023798A1 (en) * 1994-03-04 1995-09-08 Merck & Co., Inc. Prodrugs of morpholine tachykinin receptor antagonists
WO2006060110A2 (en) * 2004-11-05 2006-06-08 Merck & Co., Inc. 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
WO2010018595A2 (en) * 2008-07-17 2010-02-18 Glenmark Generics Limited Fosaprepitant dimeglumine intermediate, neutral fosaprepitant, and amorphous fosaprepitant dimeglumine and processes for their preparations

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
HALE J J ET AL: "PHOSPHORYLATED MORPHOLINE ACETAL HUMAN NEUROKININ-1 RECEPTOR ANTAGONISTS AS WATER SOLUBLE PRODRUGS", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, WASHINGTON, US, vol. 43, no. 6, 1 January 2000 (2000-01-01), pages 1234 - 1241, XP009066442, ISSN: 0022-2623, DOI: DOI:10.1021/JM990617V *

Also Published As

Publication number Publication date
WO2011045817A2 (en) 2011-04-21

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