PHENOXYACETIC ACID DERIVATIVE AND PHARMACEUTICAL PREPARATION CONTAINING THE SAME

NEW MATERIAL:A compound of formula I (X is H, halogen, lower alkyl, CF3, alkoxyhydroxyl or cyano; R1 is H, CH3 or C2H5; R2 is H or n-propyl; (n) is 0-2; (m) is 1-5) and its salt. EXAMPLE:4-[3-(4-Chlorobenzenesulfonyl)propyl]-2-[(4-acetyl-3-hydroxy-2 -propyl) phenoxyacetylamino]phenoxyacetic acid. US...

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Hauptverfasser: MAEDA SACHIKO, OZAWA SHINJI, IGARASHI AZUMA, HIRAKAWA YASUHIRO, SUGIZAKI KATSUYOSHI
Format: Patent
Sprache:eng
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Zusammenfassung:NEW MATERIAL:A compound of formula I (X is H, halogen, lower alkyl, CF3, alkoxyhydroxyl or cyano; R1 is H, CH3 or C2H5; R2 is H or n-propyl; (n) is 0-2; (m) is 1-5) and its salt. EXAMPLE:4-[3-(4-Chlorobenzenesulfonyl)propyl]-2-[(4-acetyl-3-hydroxy-2 -propyl) phenoxyacetylamino]phenoxyacetic acid. USE:A medicine; namely, thromboxane A2 antagonist, leukotriene antagonist. Usable as a preventive, active on thrombosis caused by thromboxane A2 or leukotriene, and allergies such as asthma. PREPARATION:A reaction is made in the presence of an appropriate base between a sulfonic acid derivative of formula II and a peonol derivative of formula III followed by eliminating the protecting radicals, and then reaction with ethyl bromoacetate, and the ester portion of the reaction product is put to hydrolysis with an alkali, thus obtaining the objective compound of the formula I.