| 摘要 |
<p>PROBLEM TO BE SOLVED: To obtain an arylamide of heterocyclic aromatic carboxylic acid at a nearly stoichiometric yield from an easily available heterocyclic aromatic halide by its reaction with carbon monoxide and an aromatic amine in the presence of a catalyst and a base. SOLUTION: This arylamide of heterocyclic aromatic carboxylic acid of formula IV is obtained by a reaction of a halide of formula I (A<1> is N or a CR<1> ; A<2> is N or a CR<2> ; A<3> is N or CR<3> ; A<4> is N or CR<4> ; A<5> is N or CR<5> ; R<1> -R<5> are each H, or a 1-4C alkyl or aryl; provided that at least one of A<1> -A<5> is N, and that two nitrogen atoms do not directly combine with each other; X is Cl, Br or I) with CO and an amine of formula II (R<6> is H or a 1-4C alkyl; R<7> is an aromatic group or heterocyclic aromatic group) in the presence of a base and a complex of a diphosphine of formula III (R<8> is H or a 1-4C alkyl; R<9> -R<12> are each a secondary or tertiary 3-6C alkyl, etc.; Y is O, etc.; Q is a bridged organic group, etc.) with palladium. The presence of the above- mentioned complex secures a nearly stoichiometric yield of the product of formula IV.</p> |
