选用了10种典型的P,N-双齿配体并合成相应的Au(I)配合物;以8-甲基喹啉-氮氧化物为氧化剂,Au(I)配合物/金属盐为催化剂,在氧化端炔与硫代酰胺反应制备2,4-二取代噻唑的反应中,考察了不同的金属盐对催化剂性能的影响,优化了反应参数;结果表明,5m01%Mor—DalPhosAuCl/10mol%Zn(NTf2)2催化体系在该反应中显示出了较高的催化活性,且“一步法”高效地合成了10种2,4-二取代噻唑化合物,为噻唑及其衍生物的制备探索出了一条简便直接的合成路线.
Ten typical P,N-bidentate ligands were selected to synthesize the corresponding Au(I) complexes. The catalytic system of Au(I) complex/metal salt was employed in the catalytic oxidation of terminal alkynes with the oxidant of 8-methylquinoline N-oxide. And then 2,4-disubstituted thiazoles were synthesized from the oxidized alkynes and thioamides. It was found that the catalytic system of 5 tool% Mor-DalPhosAuC1/10 mol% Zn(NTf2)2 showed the optimum catalytic perfor- mance in this reaction via adjusting reaction parameters. Furthermore, ten kinds of 2,4-disubstituted thiazoles were effectively synthesized in one-step. So a simple and direct synthetic route was explored for the preparation of thiazoles and their deriva- tives.