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WO2008003637B1 - Isolation and use of amine salts of mycophenolic acid - Google Patents

Isolation and use of amine salts of mycophenolic acid

Info

Publication number
WO2008003637B1
WO2008003637B1 PCT/EP2007/056486 EP2007056486W WO2008003637B1 WO 2008003637 B1 WO2008003637 B1 WO 2008003637B1 EP 2007056486 W EP2007056486 W EP 2007056486W WO 2008003637 B1 WO2008003637 B1 WO 2008003637B1
Authority
WO
WIPO (PCT)
Prior art keywords
mycophenolate
isolation
mycophenolic acid
water
amine salts
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/EP2007/056486
Other languages
French (fr)
Other versions
WO2008003637A2 (en
WO2008003637A3 (en
Inventor
De Robertus Mattheus Pater
Van De Emilius Johannes Sandt
Pieter Gijsbert Weber
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
DSM IP Assets BV
Original Assignee
DSM IP Assets 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
Application filed by DSM IP Assets BV filed Critical DSM IP Assets BV
Publication of WO2008003637A2 publication Critical patent/WO2008003637A2/en
Publication of WO2008003637A3 publication Critical patent/WO2008003637A3/en
Publication of WO2008003637B1 publication Critical patent/WO2008003637B1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans
    • C07D307/88—Benzo [c] furans; Hydrogenated benzo [c] furans with one oxygen atom directly attached in position 1 or 3

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

The present invention provides a method for the isolation of mycophenolic acid from a fermentation broth comprising the steps of: (a) Adding a water-immiscible solvent to said fermentation broth; (b) Separating the water-immiscible phase from the aqueous phase, and; (c) Adding an amine to the water-immiscible phase obtained in step (b). Furthermore, the present invention provides the use of mycophenolate amines in the preparation of mycophenolate esters, in particular mycophenolate mofetil, and mycophenolate salts, in particular mycophenolate sodium salt.

Claims

AMENDED CLAIMS received by the International Bureau on 25 March 2008 (25.03.2008)
9. Method according to any one of the claims 6 to 8 wherein step (d) is carries out at a temperature that is at least 0.2% below the boiling point of the mixture of components.
10. Method according to any one of the claims 6 to 9 further comprising treatment with an adsorbent.
11. Method according to any one of the claims 6 to 10 wherein said amine is triethylamine.
12. A pharmaceutical composition comprising mycophenolate mofetil obtained according to claim 11.
PCT/EP2007/056486 2006-07-05 2007-06-28 Isolation and use of amine salts of mycophenolic acid Ceased WO2008003637A2 (en)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
EP06116623 2006-07-05
EP06116621 2006-07-05
EP06116622 2006-07-05
EP06116622.9 2006-07-05
EP06116623.7 2006-07-05
EP06116621.1 2006-07-05
EP06120381 2006-09-08
EP06120381.6 2006-09-08

Publications (3)

Publication Number Publication Date
WO2008003637A2 WO2008003637A2 (en) 2008-01-10
WO2008003637A3 WO2008003637A3 (en) 2008-05-08
WO2008003637B1 true WO2008003637B1 (en) 2008-07-03

Family

ID=38537592

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2007/056486 Ceased WO2008003637A2 (en) 2006-07-05 2007-06-28 Isolation and use of amine salts of mycophenolic acid

Country Status (1)

Country Link
WO (1) WO2008003637A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100975520B1 (en) * 2008-02-01 2010-08-12 종근당바이오 주식회사 Improved Method of Making Mycophenolate Mofetil
US20110166347A1 (en) * 2008-09-10 2011-07-07 Ipca Laboratories Ltd. Process for preparation of mycophenolic acid, its salt and ester derivatives
CN115838363B (en) * 2023-01-09 2024-04-23 广东蓝宝制药有限公司 Purification method of mycophenolic acid

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4753935A (en) * 1987-01-30 1988-06-28 Syntex (U.S.A.) Inc. Morpholinoethylesters of mycophenolic acid and pharmaceutical compositions
US5247083A (en) * 1992-07-10 1993-09-21 Syntex (U.S.A.) Inc. Direct esterification of mycophenolic acid
HUP9903226A2 (en) * 1999-09-23 2002-08-28 Gyogyszerki Process for producing mycophenolic acid and derivatives thereof
EP1532130B1 (en) * 2002-08-29 2009-11-04 Biocon Limited Process for the production of an immunosuppressant
CA2537958C (en) * 2003-09-11 2013-06-11 Sandoz Ag Process for the production of mycophenolate mofetil
AU2003272083A1 (en) * 2003-10-07 2005-04-21 Biocon Limited Salt of 6-(1, 3-dihydro-4-hydroxy-6-methoxy-7-methyl-3-oxo-5-isobenzofuranyl)-4-methyl-4-hexenoic acid with n, n-dimethyl-imidodicarbonimidic diamide
JP2007532585A (en) * 2004-04-26 2007-11-15 テバ ジョジセルジャール ザ−トケルエン ムケド レ−スベニュタ−ルシャシャ−グ Method for preparing mycophenolic acid and its ester derivatives

Also Published As

Publication number Publication date
WO2008003637A2 (en) 2008-01-10
WO2008003637A3 (en) 2008-05-08

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