| 摘要 |
Prepn. of quinoline derivs. of formula (I) and their salts by reaction of a benzoxazindione (II) with a nitroacetate R2OOC-CH2-NO2 (III): (II) in the presence of a strong base. The prod. mixt. if acidified to yield the free cpd. if desired. R0=H, 1-6C alkyl, 3-6C alkenyl, or 3-6C alkynyl with the proviso that the multiple bond is not in the alpha-posn. with respect to the N at atom, 3-6C cycloalkyl, 3-6C cycloalkyl-1-2C alkyl or -(CH2)n-(C6H4.Y, Y1) where Y, Y1 independently are H, F, Cl, Br, 1-3C alkyl, 1-3C alkoxy or CF3; n=0 or 1; R, R1 independently are H, F, Cl, Br, 1-4C alkyl, 1-4C alkoxy, nitro or CF3 with the proviso that only one is CF3 or nitro and R2 is 1-5C alkyl. Cpds. (I) (where R0=alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or -CH2n-(C6H4.Y, Y1) and at least one of Y and Y1 not H or where R0=H, alkyl, phenyl or benzyl and R=CF3; R1=H, F, Cl, Br, alkyl or alkoxy or R=alkoxy, R1=H or alkoxy) and their salts are novel cpds. (I) have similar activity to that of disodium chromoglycate and in particular inhibit histamine liberation. They are useful for the treatment of allergic states such as asthma when administered orally, parenterally or rectally in daily doses of 20-200mg. A typical cpd. is 1-allyl-4-hydroxy-3-nitro-quinoline-2(1H)one. |
