QUINOLYLOXAZOLE-2-ONES USEFUL AS PROTEINKINASE C INHIBITORS

摘要

This invention relates to novel quinolyloxazole-2-ones of the formula: (I) wherein R and R1 are each independently selected from the group consisting of hydrogen, C1-C6 alkyl, and C1-C3 alkylphenyl wherein the phenyl ring is optionally substituted with one, two or three of the substituents selected from the group consisting of fluorine, chlorine, bromine, C1-C4 alkyl, and C1-C4 alkoxy; and R2 is a 2-, 3-, or 4-quinolyl group, optionally substituted with one, two or three of the substituents selected from the group consisting of fluorine, chlorine, bromine, C1-C4 alkyl, C1-C4 alkoxy, nitro and trifluoromethyl, or R2 is a 5-, 6-, 7-, or 8-quinolyl group; which are useful as protein kinase C inhibitors, effective in the treatment of hypertension and asthma. This invention also includes a novel procedure for producing an intermediate ketone compound involving the reaction of a bromo-quinoline compound with butyl lithium and further reacting the lithiated compound with N-methyl-N-methoxyalkanamide.