摘要:
ANTHELMINTICALLY ACTIVE BENZIMIDAZOLES HAVING AN OFLUORONAPHTHYL GROUP AT THE 2-POSITION ARE PREPARED BY A VARIETY OF PROCESSES INCLUDING REACTION OF AN O-NITROANILINE OR O-PHENYLENEDIAMINE WITH 3-FLUORO-2-NAPHTHOIC ACID OR AN EQUIVALENT THEREOF WHEREIN THE CARBOXYLIC ACID RADICAL IS DERIVATIZED TO A RADICAL SUCH AS AN ESTER, IMIDOESTER, AMIDE, CARBONYL HALIDE OR NITRILE.
WHEREIN R1 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND CHLORINE, R2 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND LOWER ALKOXY, R3 IS SELECTED FROM THE GROUP CONSISTING OF PIPERIDINO AND A-METHYL-BENZYLAMINO RADICALS, R4 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND METHYL RADICAL, X IS SELECTED FROM THE GROUP CONSISTING OF =O, =S, AND =NH, Y IS SELECTED FROM THE GROUP CONSISTING OF DIRECT BOND AND ALKYLENE HAVING FROM 1 TO 2 CARBON ATOMS, AND N IS SELECTED FROM THE GROUP CONSISTING OF 1 AND 2, AND THE POSITIONS OF R2 AND OF THE ETHER BOND IN THE PHENYL RADICAL ARE SELECTED FROM THE GROUP CONSISTING OF 2'', 3'', AND 4'', AND THEIR ACID ADDITION SALTS AND QUATERNARY AMMONIUM DERIVATIVES. THESE COMPOUNDS POSSESS VALUABLE PHARMACOLOGICAL PROPERTIES. THEY SHOW ANTI-ANGINOSE, CORONARY VASODILATOR AND PERIPHERAL CIRCULATION ENHANCING EFFECTS.