RU2004100227A - Способ получения микофенолят мофетила - Google Patents
Способ получения микофенолят мофетила Download PDFInfo
- Publication number
- RU2004100227A RU2004100227A RU2004100227/04A RU2004100227A RU2004100227A RU 2004100227 A RU2004100227 A RU 2004100227A RU 2004100227/04 A RU2004100227/04 A RU 2004100227/04A RU 2004100227 A RU2004100227 A RU 2004100227A RU 2004100227 A RU2004100227 A RU 2004100227A
- Authority
- RU
- Russia
- Prior art keywords
- range
- solvent
- ethers
- producing
- mycophenolat
- Prior art date
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)
- Saccharide Compounds (AREA)
- Furan Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (8)
1. Способ получения микофенолят мофетила путем прямой этерификации микофенольной кислоты и 2-морфолиноэтанола, отличающийся тем, что этерификацию проводят при кипячении в простых эфирах.
2. Способ по п.1, отличающийся тем, что используют простые эфиры в качестве растворителя с общей формулой R3OR4, где R3 и R4 независимо друг от друга означают алкил или арил.
3. Способ по п.2, отличающийся тем, что используют простые эфиры в качестве растворителя с температурой кипения выше 120°C.
4. Способ по п.1, отличающийся тем, что используют от 1,01 до 3,0 молярных эквивалентов 2-морфолиноэтанола.
5. Способ по п.3, отличающийся тем, что используют дибутиловый эфир в качестве инертного растворителя.
6. Способ по п.5, отличающийся тем, что начальная температура реакции находится в диапазоне 130-138°C, и конечная температура реакции находится в диапазоне 140-145°C.
7. Способ по п.5, отличающийся тем, что время кипячения находится в пределах от 30 до 80 ч.
8. Способ по п.5, отличающийся тем, что соотношение микофенольной кислоты и растворителя находится в интервале от 1 г/2 мл до 1 г/5 мл.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CZ20012071A CZ292123B6 (cs) | 2001-06-08 | 2001-06-08 | Způsob přípravy mykofenolátu mofetilu |
| CZPV2001-2071 | 2001-06-08 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2004100227A true RU2004100227A (ru) | 2005-06-27 |
| RU2283313C2 RU2283313C2 (ru) | 2006-09-10 |
Family
ID=5473426
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2004100227/04A RU2283313C2 (ru) | 2001-06-08 | 2002-06-08 | Способ получения микофенолят мофетила |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US20050085635A1 (ru) |
| EP (1) | EP1421081A4 (ru) |
| JP (1) | JP2004534063A (ru) |
| KR (1) | KR20040030660A (ru) |
| CN (1) | CN1253450C (ru) |
| AR (1) | AR041777A1 (ru) |
| BR (1) | BR0210931A (ru) |
| CA (1) | CA2450013A1 (ru) |
| CZ (1) | CZ292123B6 (ru) |
| HK (1) | HK1068630A1 (ru) |
| HU (1) | HUP0400189A3 (ru) |
| NZ (1) | NZ530013A (ru) |
| PL (1) | PL364366A1 (ru) |
| RU (1) | RU2283313C2 (ru) |
| SK (1) | SK285663B6 (ru) |
| TW (1) | TWI241299B (ru) |
| WO (1) | WO2002100855A1 (ru) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1667987B1 (en) * | 2003-09-11 | 2008-07-23 | Sandoz AG | Process for the production of mycophenolate mofetil |
| US7683188B2 (en) | 2004-04-26 | 2010-03-23 | TEVA Gyógyszergyár Zártkōrūen Mūkōdō Részvénytársaság | Process for preparation of mycophenolic acid and ester derivatives thereof |
| CA2555454C (en) | 2004-04-27 | 2009-12-15 | Sandor Molnar | Mycophenolate mofetil impurity |
| CN101014584A (zh) | 2004-07-20 | 2007-08-08 | 特瓦药厂私人有限公司 | 结晶霉酚酸钠的制备方法 |
| 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 |
| DK2032712T3 (da) * | 2006-06-29 | 2010-05-25 | Ivax Pharmaceuticals Sro | Regulering af syremetabolitproduktion |
| 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 |
| TW200904982A (en) * | 2007-04-11 | 2009-02-01 | Teva Gyogyszergyar Zartkoruen Mukodo Reszvenytarsasag | Method for reducing impurity level in mycophenolic acid fermentation |
| WO2009000834A1 (en) * | 2007-06-27 | 2008-12-31 | Dsm Ip Assets 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)
| 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 |
-
2001
- 2001-06-08 CZ CZ20012071A patent/CZ292123B6/cs not_active IP Right Cessation
-
2002
- 2002-06-07 AR ARP020102144A patent/AR041777A1/es not_active Application Discontinuation
- 2002-06-07 TW TW091112451A patent/TWI241299B/zh not_active IP Right Cessation
- 2002-06-08 WO PCT/US2002/018274 patent/WO2002100855A1/en active IP Right Grant
- 2002-06-08 EP EP02756146A patent/EP1421081A4/en not_active Withdrawn
- 2002-06-08 KR KR10-2003-7016069A patent/KR20040030660A/ko not_active Application Discontinuation
- 2002-06-08 PL PL02364366A patent/PL364366A1/xx unknown
- 2002-06-08 US US10/480,058 patent/US20050085635A1/en not_active Abandoned
- 2002-06-08 NZ NZ530013A patent/NZ530013A/en unknown
- 2002-06-08 SK SK1506-2003A patent/SK285663B6/sk unknown
- 2002-06-08 HU HU0400189A patent/HUP0400189A3/hu unknown
- 2002-06-08 BR BR0210931-0A patent/BR0210931A/pt not_active IP Right Cessation
- 2002-06-08 CN CNB028126998A patent/CN1253450C/zh not_active Expired - Fee Related
- 2002-06-08 JP JP2003503622A patent/JP2004534063A/ja active Pending
- 2002-06-08 RU RU2004100227/04A patent/RU2283313C2/ru not_active IP Right Cessation
- 2002-06-08 CA CA002450013A patent/CA2450013A1/en not_active Abandoned
-
2005
- 2005-02-18 HK HK05101061A patent/HK1068630A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2002100855A1 (en) | 2002-12-19 |
| BR0210931A (pt) | 2004-06-08 |
| HUP0400189A3 (en) | 2007-05-29 |
| CA2450013A1 (en) | 2002-12-19 |
| CZ20012071A3 (cs) | 2003-01-15 |
| CZ292123B6 (cs) | 2003-08-13 |
| HK1068630A1 (en) | 2005-04-29 |
| SK285663B6 (sk) | 2007-05-03 |
| KR20040030660A (ko) | 2004-04-09 |
| NZ530013A (en) | 2005-05-27 |
| SK15062003A3 (en) | 2004-11-03 |
| CN1253450C (zh) | 2006-04-26 |
| EP1421081A4 (en) | 2004-11-03 |
| HUP0400189A2 (hu) | 2004-07-28 |
| AR041777A1 (es) | 2005-06-01 |
| JP2004534063A (ja) | 2004-11-11 |
| RU2283313C2 (ru) | 2006-09-10 |
| PL364366A1 (en) | 2004-12-13 |
| EP1421081A1 (en) | 2004-05-26 |
| TWI241299B (en) | 2005-10-11 |
| US20050085635A1 (en) | 2005-04-21 |
| CN1520411A (zh) | 2004-08-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20080609 |