AR041777A1 - Proceso de preparacion de micofenolato mofetilo - Google Patents

Proceso de preparacion de micofenolato mofetilo

Info

Publication number
AR041777A1
AR041777A1 ARP020102144A ARP020102144A AR041777A1 AR 041777 A1 AR041777 A1 AR 041777A1 AR P020102144 A ARP020102144 A AR P020102144A AR P020102144 A ARP020102144 A AR P020102144A AR 041777 A1 AR041777 A1 AR 041777A1
Authority
AR
Argentina
Prior art keywords
mycophenolate
solvents
mofetilo
ethers
preparation process
Prior art date
Application number
ARP020102144A
Other languages
English (en)
Inventor
M Chudik
A Husek
Original Assignee
Ivax Cr A S
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 Ivax Cr A S filed Critical Ivax Cr A S
Publication of AR041777A1 publication Critical patent/AR041777A1/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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • 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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Furan Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)

Abstract

Un proceso de preparación de micofenolato de fórmula (1): donde R1 = 2-(4morfolinil)etilo y R2 = átomo de hidrógeno, por esterificación directa de ácido microfenólico con 2 morfolino etanol, donde la esterificación se lleva a cabo bajo ebullición en éteres como solventes, de fórmula general R3OR4 donde R3 y R4 son independientemente alquilo o arilo. Preferentemente, los éteres empleados como solventes poseen un punto de ebullición superior a 120°C y la concentración de 2-morfolino etanol oscila entre 1,01 a 3 equivalentes molares. El microfenolato mofetilo se usa como inmunosupresor para el tratamiento profiláctico en combinación con otros inmunosupresores (ciclosporina A, prednisonal) o para el tratamiento de rechazos refractorios en pacientes luego de un transplante renal.
ARP020102144A 2001-06-08 2002-06-07 Proceso de preparacion de micofenolato mofetilo AR041777A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CZ20012071A CZ292123B6 (cs) 2001-06-08 2001-06-08 Způsob přípravy mykofenolátu mofetilu

Publications (1)

Publication Number Publication Date
AR041777A1 true AR041777A1 (es) 2005-06-01

Family

ID=5473426

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020102144A AR041777A1 (es) 2001-06-08 2002-06-07 Proceso de preparacion de micofenolato mofetilo

Country Status (17)

Country Link
US (1) US20050085635A1 (es)
EP (1) EP1421081A4 (es)
JP (1) JP2004534063A (es)
KR (1) KR20040030660A (es)
CN (1) CN1253450C (es)
AR (1) AR041777A1 (es)
BR (1) BR0210931A (es)
CA (1) CA2450013A1 (es)
CZ (1) CZ292123B6 (es)
HK (1) HK1068630A1 (es)
HU (1) HUP0400189A3 (es)
NZ (1) NZ530013A (es)
PL (1) PL364366A1 (es)
RU (1) RU2283313C2 (es)
SK (1) SK285663B6 (es)
TW (1) TWI241299B (es)
WO (1) WO2002100855A1 (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE402157T1 (de) * 2003-09-11 2008-08-15 Sandoz Ag Verfahren zur herstellung von mycophenolatmofetil
WO2005105768A2 (en) * 2004-04-26 2005-11-10 Teva Gyógyszergyár Zàrtköruen Muködo Rèszvènytàrsasàg Process for preparation of mycophenolic acid and ester derivatives thereof
WO2005105769A2 (en) 2004-04-27 2005-11-10 Teva Gyógyszergyár Zàrtköruen Muködo Rèszvènytàrsasàg - Mycophenolate mofetil impurity
CA2573781A1 (en) 2004-07-20 2006-02-02 Teva Gyogyszergyar Zartkoruen Mukodo Reszvenytarsasag Processes for preparation of crystalline mycophenolate sodium
ITMI20041703A1 (it) * 2004-09-03 2004-12-03 Poli Ind Chimica Spa Metodo di preparazione del mofetil micofenolato per transesterificazione enzimatica
CN1328272C (zh) * 2005-08-22 2007-07-25 鲁南制药集团股份有限公司 一种工业化生产霉酚酸莫啡酯的方法
CN100402516C (zh) * 2005-10-18 2008-07-16 深圳市东阳光实业发展有限公司 一种霉酚酸莫啡酯的制备方法
US20080009050A1 (en) * 2006-06-29 2008-01-10 Zdenek Pokluda Regulation of acid metabolite production
CN1974564B (zh) * 2006-12-15 2010-05-12 丽珠集团新北江制药股份有限公司 一种霉酚酸莫啡酯的制备方法
US20080188653A1 (en) 2007-02-04 2008-08-07 Formosa Laboratories, Inc. Process for Preparation of Mycophenolate Mofetil
CN100484930C (zh) * 2007-03-16 2009-05-06 重庆大新药业股份有限公司 一种吗替麦考酚酯的制备方法
EP2024506A1 (en) * 2007-04-11 2009-02-18 Teva Gyógyszergyár Zártköruen Muködo Részvénytársaság Method for reducing impurity level in mycophenolic acid fermentation
US8273739B2 (en) 2007-06-27 2012-09-25 Dsm Sinochem Pharmaceuticals Netherlands B.V. Method for the purification of mycophenolate mofetil
WO2009003878A1 (en) * 2007-06-29 2009-01-08 Dsm Ip Assets B.V. Method for the preparation of mycophenolate mofetil
WO2009010503A1 (en) * 2007-07-18 2009-01-22 Dsm Ip Assets B.V. Mycophenolic acid recycling in a method for the preparation of mycophenolate mofetil
CN101671706B (zh) * 2009-09-05 2013-09-18 山东新时代药业有限公司 一种霉酚酸发酵过程中补糖方法
CN103265514B (zh) * 2013-06-08 2016-01-13 重庆理工大学 一种制备吗替麦考酚酯的方法
CN107056736A (zh) * 2017-05-08 2017-08-18 福建省微生物研究所 一种吗替麦考酚酯的制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4748173A (en) * 1987-01-30 1988-05-31 Syntex (U.S.A.) Inc. Heterocyclic aminoalkyl esters of mycophenolic acid and derivatives thereof and pharmaceutical compositions
HU203678B (en) * 1988-09-26 1991-09-30 Richter Gedeon Vegyeszet Method for increased dewatering condensation reaction mixtures
US5247083A (en) * 1992-07-10 1993-09-21 Syntex (U.S.A.) Inc. Direct esterification of mycophenolic acid

Also Published As

Publication number Publication date
CA2450013A1 (en) 2002-12-19
RU2283313C2 (ru) 2006-09-10
CZ20012071A3 (cs) 2003-01-15
TWI241299B (en) 2005-10-11
BR0210931A (pt) 2004-06-08
CN1520411A (zh) 2004-08-11
CZ292123B6 (cs) 2003-08-13
CN1253450C (zh) 2006-04-26
SK285663B6 (sk) 2007-05-03
HUP0400189A3 (en) 2007-05-29
HUP0400189A2 (hu) 2004-07-28
EP1421081A1 (en) 2004-05-26
JP2004534063A (ja) 2004-11-11
US20050085635A1 (en) 2005-04-21
RU2004100227A (ru) 2005-06-27
NZ530013A (en) 2005-05-27
HK1068630A1 (en) 2005-04-29
WO2002100855A1 (en) 2002-12-19
KR20040030660A (ko) 2004-04-09
SK15062003A3 (en) 2004-11-03
PL364366A1 (en) 2004-12-13
EP1421081A4 (en) 2004-11-03

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