| 摘要 |
The invention relates to a novel process for the preparation of 4-azaphthalide compounds of the formula <IMAGE> in which Y is hydrogen, C1-C12 alkyl which is unsubstituted or substituted by halogen, cyano, hydroxyl or lower alkoxy, acyl having 1 to 12 carbon atoms, benzyl or benzyl which is substituted by halogen, nitro, lower alkyl or lower alkoxy, Z is hydrogen, lower alkyl or phenyl, X is -OR1 or, <IMAGE> R1 and R2 independently of each other are hydrogen, C1-C12 alkyl which is unsubstituted or substituted by halogen, cyano, hydroxyl or lower alkoxy, cycloalkyl, phenyl, benzyl or phenyl or benzyl which is substituted by halogen, nitro, cyano, lower alkyl, lower alkoxy or lower alkoxycarbonyl, or R1 and R2 together with the connecting nitrogen atom, are a 5-membered or 6-membered heterocyclic radical and V is hydrogen, halogen hydroxyl, nitro, lower alkyl or lower alkoxy, and in which the ring A is unsubstituted or substituted by halogen, nitro, cyano, lower alkyl, lower alkoxy, lower alkoxycarbonyl, amino, mono-(lower alkyl)-amino or di-(lower alkyl)-amino, which process comprises reacting quinolic anhydride with an indole compound of the formula <IMAGE> in which A, Y and Z are as defined, in the presence of an inorganic or organic metal salt of a polyvalent metal in an organic reaction medium consisting of a lower aliphatic monocarboxylic acid or a nitrile of this acid at a temperature of not more than 65 DEG C, further condensing the resulting reaction product with a compound of the formula <IMAGE> in which X and V are as defined, and adjusting the pH value of the reaction mixture to not less than 6. |
