利用吲哚-2-酰胺和苯基炔丙醇为原料,在三氟甲磺酸铜[Cu(OTf)_(2)]催化下,成功构建了吲哚并氮杂卓酮类化合物。该方法实现了吲哚C-3位和酰胺N—H的官能团化,表现出优异化学选择性。通过^(1)H NMR、^(13) C NMR和HRMS对所得化合物的结构...利用吲哚-2-酰胺和苯基炔丙醇为原料,在三氟甲磺酸铜[Cu(OTf)_(2)]催化下,成功构建了吲哚并氮杂卓酮类化合物。该方法实现了吲哚C-3位和酰胺N—H的官能团化,表现出优异化学选择性。通过^(1)H NMR、^(13) C NMR和HRMS对所得化合物的结构进行了表征。实验最优条件为:反应温度60℃,反应时间5 h,溶剂1,2-二氯乙烷(DCE),5 mol%Cu(OTf)_(2),吲哚-2-酰胺:苯基炔丙醇为1∶1.2,收率73%。展开更多
Recently, it has been reported that the luteolytic ac-tion was the main mechanism of the termination of earlypregnancy by contraceptivest. In addition, some estro-gen receptor ligands such as droloxifene have beenshow...Recently, it has been reported that the luteolytic ac-tion was the main mechanism of the termination of earlypregnancy by contraceptivest. In addition, some estro-gen receptor ligands such as droloxifene have beenshown to inhibit the growth of cultured rat luteal cells.It has been known that 2-phenylindole derivatives couldcompete with estradiol for the estrogen receptor. Theseresults prompted us to design and synthesize the follow-ing six new 3-oxamoyl-2-phenylindole compounds 1a-fand test their effects on the growth of luteal cells, aimingat seeking new lead compounds possessing antifertility activities.展开更多
文摘Recently, it has been reported that the luteolytic ac-tion was the main mechanism of the termination of earlypregnancy by contraceptivest. In addition, some estro-gen receptor ligands such as droloxifene have beenshown to inhibit the growth of cultured rat luteal cells.It has been known that 2-phenylindole derivatives couldcompete with estradiol for the estrogen receptor. Theseresults prompted us to design and synthesize the follow-ing six new 3-oxamoyl-2-phenylindole compounds 1a-fand test their effects on the growth of luteal cells, aimingat seeking new lead compounds possessing antifertility activities.
