| 摘要 |
NEW MATERIAL:A compound of formula I [X1-X3 are halogen; R1 is amino, mono- or disubstituted amino, substituted or unsubstituted cyclic amino; R2 is lower alkyl, lower alkenyl, cycloalkyl, substituted or unsubstituted phenyl; R3 is H, lower alkyl; where X1 and X3 are H; the cases where X2 is Cl; R is amino; R2 is ethyl are excluded]. EXAMPLE:5-Amino-1-cyclopropyl-6,7,8-trifluoro-1,4-dihydro-4-oxoq-uinol ine-3-car boxylic acid. USE:A synthetic intermediate of a quinolonecarboxylic acid derivative of formula II (R=R1) which has strong fungicidal activity. PREPARATION:A compound of formula III (Y is halogen; R3' is lower alkyl) is allowed to react with an amine of the formula: R1-H in an inert solvent, when needed, in the presence of an acid acceptor to give a compound of formula I where R3 is R3'. The product is hydrolyzed to give the compound of formula I where R3 is H. |
