METHOD FOR PRODUCING AMINOALKOXYCARBOSTYRYL DERIVATIVE
PROBLEM TO BE SOLVED: To obtain a high-purity aminoalkoxycarbostyryl derivative by an industrially producible simple operation. SOLUTION: A phthalimidealkoxycarbostyryl derivative is heated in the presence of a basic compound to afford a phthalimidic acid derivative, and then, an acidic compound is added to the phthalimidic acid derivative and these compounds are heated to provide the aminoalkoxycarbostyryl derivative. Crystallization is carried out by adding an organic solvent to the reaction liquid to provide a salt of the aminoalkoxycarbostyryl derivative.
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2(1H)-Quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activities
In order to search for anti-arteriostenotic agents, a series of 2(1H)- quinolinone derivatives was synthesized and evaluated for anti-thrombotic activity and for anti-hyperplastic activity. From this series, (-)-6-[3-[3- cyclopropyl-3-[(1R,2R)-2-hydroxycycyclohexyl]ureido]propoxy]-2(1H)- quinolinone (1p, OPC-33509) was selected as the best candidate by balancing the efficacy on anti-thrombosis and anti-hyperplasia.