JPS57183776A - Preparation of mycophenolic acid derivative - Google Patents

Preparation of mycophenolic acid derivative

Info

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
Application number
JP6649481A
Other languages
Japanese (ja)
Inventor
Kazufumi Yagyu
Arahiko Eguchi
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.)
Ajinomoto Co Inc
Original Assignee
Ajinomoto Co Inc
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 Ajinomoto Co Inc filed Critical Ajinomoto Co Inc
Priority to JP6649481A priority Critical patent/JPS57183776A/en
Publication of JPS57183776A publication Critical patent/JPS57183776A/en
Pending legal-status Critical Current

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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
JP6649481A 1981-05-01 1981-05-01 Preparation of mycophenolic acid derivative Pending JPS57183776A (en)

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)

* Cited by examiner, † Cited by third party
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

Cited By (8)

* Cited by examiner, † Cited by third party
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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