JPS57183776A - Preparation of mycophenolic acid derivative - Google Patents
Preparation of mycophenolic acid derivativeInfo
- Publication number
- JPS57183776A JPS57183776A JP6649481A JP6649481A JPS57183776A JP S57183776 A JPS57183776 A JP S57183776A JP 6649481 A JP6649481 A JP 6649481A JP 6649481 A JP6649481 A JP 6649481A JP S57183776 A JPS57183776 A JP S57183776A
- Authority
- JP
- Japan
- Prior art keywords
- mycophenolic acid
- acid derivative
- reacting
- alkyl
- active hydrogen
- 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.)
- Pending
Links
Landscapes
- Furan Compounds (AREA)
Abstract
PURPOSE: To prepare a mycophenolic acid derivative useful especially as a drug such as carcinostatic agent, etc., economically, in an industrial scale, by reacting a mycophenolic acid ester with an isocyanate compound in the presence of an organic amine devoid of active hydrogen.
CONSTITUTION: The mycophenolic acid derivative of formula III (R is alkyl; R1 is alkyl, aryl or aralkyl, all of which may have substituent groups) can be prepared economically, without directly using highly toxic phosgene, by reacting the mycophenolic acid ester of formulaIwith the isocyanate compound of formula II in the presence of an organic amine having no active hydrogen atom in the molecule, e.g. trimethylamine, triethylamine, pyridine, 2,6-lutidine, N-methylmorpholine, N,N-dimethylaniline, etc. The amount of the amine is stoichiometric or more, based on the compound of formulaI.
COPYRIGHT: (C)1982,JPO&Japio
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP6649481A JPS57183776A (en) | 1981-05-01 | 1981-05-01 | Preparation of mycophenolic acid derivative |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP6649481A JPS57183776A (en) | 1981-05-01 | 1981-05-01 | Preparation of mycophenolic acid derivative |
Publications (1)
Publication Number | Publication Date |
---|---|
JPS57183776A true JPS57183776A (en) | 1982-11-12 |
Family
ID=13317411
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP6649481A Pending JPS57183776A (en) | 1981-05-01 | 1981-05-01 | Preparation of mycophenolic acid derivative |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS57183776A (en) |
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4686234A (en) * | 1985-11-27 | 1987-08-11 | Syntex (U.S.A) Inc. | Mycophenolic acid derivatives in the treatment of inflammatory diseases, in particular rheumatoid arthritis |
US4725622A (en) * | 1986-01-23 | 1988-02-16 | Syntex (U.S.A.) Inc. | Mycophenolic acid derivatives in the treatment of rheumatoid arthritis |
US4868153A (en) * | 1987-01-30 | 1989-09-19 | Syntex (U.S.A.) Inc. | Treatment of allograft rejection with mycophenolic acid, its morpholinoethylester and derivatives thereof |
US4959387A (en) * | 1986-01-23 | 1990-09-25 | Syntex (U.S.A.) Inc. | Mycophenolic acid derivatives in the treatment of rheumatoid arthritis |
US5177072A (en) * | 1987-01-30 | 1993-01-05 | Syntex (U.S.A.) Inc. | Treatment of autoimmune inflammatory, and psoriatic diseases with heterocyclic aminoalkyl esters of mycophenolic acid and derivatives |
-
1981
- 1981-05-01 JP JP6649481A patent/JPS57183776A/en active Pending
Cited By (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4686234A (en) * | 1985-11-27 | 1987-08-11 | Syntex (U.S.A) Inc. | Mycophenolic acid derivatives in the treatment of inflammatory diseases, in particular rheumatoid arthritis |
US4725622A (en) * | 1986-01-23 | 1988-02-16 | Syntex (U.S.A.) Inc. | Mycophenolic acid derivatives in the treatment of rheumatoid arthritis |
US4959387A (en) * | 1986-01-23 | 1990-09-25 | Syntex (U.S.A.) Inc. | Mycophenolic acid derivatives in the treatment of rheumatoid arthritis |
US4868153A (en) * | 1987-01-30 | 1989-09-19 | Syntex (U.S.A.) Inc. | Treatment of allograft rejection with mycophenolic acid, its morpholinoethylester and derivatives thereof |
US4948793A (en) * | 1987-01-30 | 1990-08-14 | Syntex (U.S.A.) Inc. | Treatment of autoimmune diseases with the morpholinoethyl ester of mycophenolic acid, and derivatives thereof |
US4952579A (en) * | 1987-01-30 | 1990-08-28 | Syntex (U.S.A.) Inc. | Method of treating diseases by administering morpholino-ethylester of mycophenolic acid or derivatives thereof |
US4992467A (en) * | 1987-01-30 | 1991-02-12 | Syntex (U.S.A.) Inc. | Treatment of autoimmune diseases with mycophenolic acid, and derivatives and formulations thereof |
US5177072A (en) * | 1987-01-30 | 1993-01-05 | Syntex (U.S.A.) Inc. | Treatment of autoimmune inflammatory, and psoriatic diseases with heterocyclic aminoalkyl esters of mycophenolic acid and derivatives |
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