| 摘要 |
<p>1411625 7 - Aminoindazole derivatives WANDER Ltd 28 Nov 1972 [1 Dec 1971 12 Oct 1972] 54871/72 Heading C2C Novel compounds of Formula I wherein R 1 is hydrogen or alkyl of 1 to 3 carbon atoms, R 2 is hydrogen, fluorine, chlorine, bromine, or alkyl, alkoxy or alkylthio of 1 to 3 carbon atoms, R 3 is hydrogen, fluorine, chlorine, bromine, alkyl or alkoxy of 1 to 3 carbon atoms, or hydroxy, and A is dimethylene, trimethylene, hydroxydimethylene, hydroxytrimethylene, alkyl-dimethylene of 3 to 5 carbon atoms or alkyl-trimethylene of 4 to 6 carbon atoms are prepared by one of the following methods (a) a compound of Formula II wherein R 4 is -S-R 5 , O-R 5 or -NHNO 2 where R 5 is H or C 1-5 alkyl is reacted with a compound NH 2 -A-NH 2 ; (b) a compound of Formula V is cyclized; or (c) a compound of Formula IV is reacted with a compound of formula Intermediates of Formula II above are prepared by reaction of benzyl chloride and ammonium thiocyanate with a compound of Formula IV, above, which is obtained by reduction of the corresponding nitro compound which is obtained by ring alkylation of the indazole. Intermediates of Formula V above are prepared by reaction of a compound of Formula IV above with thiophosgene and NH 2 ANH 2 . Intermediates of Formula IV above are prepared by reaction of lead acetate and potassium hydroxide on the 7-thiourea compound. Pharmaceutical compositions in conventional forms for oral administration having analgesic activity and some with antihypertensive activity comprise an above novel compound and a carrier or diluent.</p> |
