A comparative study of conventional conditions versus microwave irradiation for the preparation of novel 1,2-dihydro-2-imino-7-methyl-1,6(6<i>H</i>)-naphthyridin-5-ones
作者:Dieter Heber、Edmont V. Stoyanov
DOI:10.1002/jhet.5570370432
日期:2000.7
The synthesis of novel 1,6-naphthyridines 6 with potential activity against tuberculosis is described using the reaction sequence 2←4←6. Depending on the ring N-substitution of the 4-alkylamino-6-methyl-2(1H)-pyridones 1 and 2 the electrophilic attack of the Vilsmeier reagent gives rise to the formation of the exocyclic N-formyl derivatives 3 from 1 and the corresponding 3-carbaldehydes 4 from 2. 1
使用反应序列2←4←6描述了具有潜在抗结核活性的新型1,6-萘啶6的合成。取决于环Ñ 4烷基氨基-6-甲基-2(1的3'-取代ħ) -吡啶酮1和2的Vilsmeier试剂的亲电攻击引起环外形成Ñ甲酰基衍生物3从1和相应的3- carbaldehydes 4从2 1,2-二氢-2-亚氨基-7-甲基-1,6-(6 ħ) -萘啶-5-酮6A-J是由的Knoevenagel反应制备4用CH-酸性腈5.这些反应进行了使用的常规条件下(室温或回流下)相对于微波辐射的比较研究。