主权项 |
1. A process for preparing a compound of formula (III) in which Ar is agroup,
where R1, R2, R3, R4 and R5 are the same or different and are each independently hydrogen, amino, cyano, nitro, halogen, optionally halogen-substituted C1-C6-alkyl, C1-C6-thioalkyl, thiophenyl, C1-C6-alkoxy, C6-C10-aryloxy, phenyl, —CO—C6-C10-aryl, —CO—C1-C3-alkyl, —COO—C1-C6-alkyl or —COO—C6-C10-aryl, the Ar radical may additionally also be a heteroaromatic radical or the Ar radical may also be 1- or 2-naphthyl, and R6 and R7 are each independently optionally substituted C1-C8-alkyl, phenyl, aryl, or NR8R9, where R8 and R9 are the same or different and are each independently C1-C4-alkyl, or phenyl optionally substituted by optionally fluorine- or chlorine-substituted C1-C3-alkyl, by nitro, cyano or di-C1-C3-alkylamino, or together with the nitrogen atom to which they are bonded are a saturated or unsaturated, substituted or unsubstituted cycle, wherein an aryl or heteroaryl halide of formula (I)
Ar-Hal (I) in which Hal is chlorine, bromine or iodine and Ar is as defined above, is reacted with a malonic ester of formula (II) in the presence of a palladium catalyst, of a phosphine ligand and of a mixture of inorganic bases, without using caesium carbonate or caesium bicarbonate, wherein the mixture of inorganic bases comprises potassium carbonate and potassium bicarbonate in a ratio of 1:1, optionally using an organic solvent. |