Process for the preparation of 2-substituted and 2,3-disubstitut

Details Process for the preparation of 2-substituted and 2,3-disubstitut Process for the preparation of 2-substituted and 2,3-disubstitut

1992-11-04

1995-03-21

Springer, David B.

Textiles: spinning, twisting, and twining

548466, 548544, 548552, 548527, C07D40314, C07D40304, C07D207456, C07D40904

Patent

active

053997123

ABSTRACT:
The invention relates to a process for the manufacture of substituted maleimides of the formula ##STR1## wherein R.sup.1 is alkyl, aryl or heteroaryl and R.sup.2 is hydrogen, alkyl, alkoxycarbonyl, aryl or heteroaryl, by reacting an activated glyoxylate of the formula ##STR2## wherein R.sup.1 has the above significance and X is a leaving atom or group,
with an imidate of the formula ##STR3## wherein R.sup.2 has the above significance, R.sup.3 is alkyl, aryl or trialkylsilyl and Y is oxygen or sulfur, in the presence of a base and, after treating the resulting reaction product obtained in which R.sup.2 is hydrogen or alkyl with a strong base, hydrolyzing and dehydrating the resulting hydroxy-pyrrolinone of the formula ##STR4## wherein R.sup.1, R.sup.2, R.sup.3 and Y have the above significance. The substituted maleimides of formula I are pharmacologically active, for example as protein kinase C inhibitors and which a useful, for example, in the treatment and prophylaxis of inflammatory, immunological, bronchopulmonary and cardiovascular disorders, or as antiproliferative agents useful, for example, in the treatment of immune diseases and allergic disorders.

REFERENCES:
patent: 4332822 (1982-06-01), Ward
patent: 4886908 (1989-12-01), Haeusler
patent: 4962204 (1990-10-01), Wambach
patent: 5057614 (1991-10-01), Davis et al.

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