AR074230A1 - PROCESS TO PREPARE ZOLEDRONIC ACID - Google Patents

PROCESS TO PREPARE ZOLEDRONIC ACID

Info

Publication number
AR074230A1
AR074230A1 ARP090104567A ARP090104567A AR074230A1 AR 074230 A1 AR074230 A1 AR 074230A1 AR P090104567 A ARP090104567 A AR P090104567A AR P090104567 A ARP090104567 A AR P090104567A AR 074230 A1 AR074230 A1 AR 074230A1
Authority
AR
Argentina
Prior art keywords
intermediates
formula
prepare
zoledronic acid
salt
Prior art date
Application number
ARP090104567A
Other languages
Spanish (es)
Inventor
Martin Kas
Jaroslav Pis
Michal Benes
Original Assignee
Synthon Bv
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
Priority claimed from EP08075904A external-priority patent/EP2192126B1/en
Application filed by Synthon Bv filed Critical Synthon Bv
Publication of AR074230A1 publication Critical patent/AR074230A1/en

Links

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
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503—Five-membered rings
    • C07F9/6506—Five-membered rings having the nitrogen atoms in positions 1 and 3

Landscapes

  • 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)

Abstract

La invencion se relaciona con un proceso, el cual comprende: hacer reaccionar en un solvente/diluyente un compuesto de formula (2) o una sal o éster del mismo con un agente de fosfonacion para formar intermediarios fosfonados, y subsiguientemente hidrolizar dichos intermediarios para formar un compuesto de formula (1) o una sal o hidrato del mismo en donde dicho solvente/diluyente comprende una mezcla de (i) un polialquilenglicol y (ii) un carbonato cíclico de la formula (3) en donde n es un entero desde 2 a 4, y R1 y R2 cada uno independientemente representan hidrogeno o un grupo alquilo C1-4 y al uso de intermediaros en el mismo.The invention relates to a process, which comprises: reacting in a solvent / diluent a compound of formula (2) or a salt or ester thereof with a phosphonation agent to form phosphonated intermediates, and subsequently hydrolyzing said intermediates to form a compound of formula (1) or a salt or hydrate thereof wherein said solvent / diluent comprises a mixture of (i) a polyalkylene glycol and (ii) a cyclic carbonate of the formula (3) wherein n is an integer from 2 at 4, and R1 and R2 each independently represent hydrogen or a C1-4 alkyl group and the use of intermediates therein.

ARP090104567A 2008-11-26 2009-11-26 PROCESS TO PREPARE ZOLEDRONIC ACID AR074230A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US11805008P 2008-11-26 2008-11-26
EP08075904A EP2192126B1 (en) 2008-11-26 2008-11-26 Process for making zoledronic acid

Publications (1)

Publication Number Publication Date
AR074230A1 true AR074230A1 (en) 2010-12-29

Family

ID=41402559

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090104567A AR074230A1 (en) 2008-11-26 2009-11-26 PROCESS TO PREPARE ZOLEDRONIC ACID

Country Status (2)

Country Link
AR (1) AR074230A1 (en)
WO (1) WO2010060619A1 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9169279B2 (en) 2009-07-31 2015-10-27 Thar Pharmaceuticals, Inc. Crystallization method and bioavailability
CA2769633C (en) 2009-07-31 2017-06-06 Thar Pharmaceuticals, Inc. Crystallization method and bioavailability
US20160016982A1 (en) 2009-07-31 2016-01-21 Thar Pharmaceuticals, Inc. Crystallization method and bioavailability
EA201270328A1 (en) * 2009-08-28 2012-09-28 Синтон Б. В. METHOD OF OBTAINING 1-HYDROXYLKYLIDENE-1,1-DIPHOSPHONE ACIDS
US9340565B2 (en) 2010-11-24 2016-05-17 Thar Pharmaceuticals, Inc. Crystalline forms
US10195218B2 (en) 2016-05-31 2019-02-05 Grunenthal Gmbh Crystallization method and bioavailability
CN111303040A (en) * 2020-03-25 2020-06-19 武汉工程大学 Method for preparing imidazole-1-acetic acid by one-pot method

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2197267C (en) * 1997-02-11 2000-02-08 Yong Tao Process for the production of 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid or salts thereof
PL373574A1 (en) * 2002-05-17 2005-09-05 Teva Pharmaceutical Industries Ltd. Use of certain diluents for making bisphosphonic acids
WO2005063717A1 (en) * 2003-12-26 2005-07-14 Natco Pharma Limited An improved process for the preparation of zoledronic acid

Also Published As

Publication number Publication date
WO2010060619A1 (en) 2010-06-03

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