研究了一种新颖的醋酸铜促进的芳基磺酰肼的自身偶联反应.该反应通过分子问脱硫和脱氮的过程,高选择性高产率的合成对称的二芳基砜类化合物.该反应中溶剂对反应的副产物的产生有十分显著的影响.反应无需惰性气体保护,具有良好的官能团耐受性,硝基、卤素等官能团及杂环体系都对反应无明显影响.该合成方法可以用于治疗麻风病的药物氨苯砜的制备.
A new homocoupling pattern with arylsulfonyl hydrazides promoted by Cu(OAc)2 is described. This transforma- tion is proceeded via intermolecular denitrification and desulfitation. Symmetrical diaryl sulfone derivatives were obtained with high selectivity and reactivity. The solvents showed striking influence to the formation of distinctive by-products. The reported homocoupling reactions are very practical as it does not require the protection of inert gas and tolerant to the many functional groups, especially nitro, halogen and heterocyclic system. The synthetic method has been applied to the synthesis of dapsone.