中文摘要：

以氯化亚铜为催化剂,叔胺为底物,磺酰叠氮为氮源,经“一锅法”合成了11个磺酰脒衍生物（3a ～3k,其中3c,3e ～3i和3k为新化合物）,收率43％～96％,其结构经1 H NMR,13C NMR和HR-ESI-MS表征.采用MTT法研究了3a～3j对人肺癌细胞（A549）,人结肠癌细胞（HCT116）和人肝癌细胞（HepG2）的抗肿瘤活性.结果表明：在用药量为20 μg·mL-1时,3a ～3k对A549,HCT116和HepG2的抑制率均优于对照药紫杉醇,其中N,N-二乙基-N’-对甲氧基苯磺酰脒（3b）对A549的抑制率为82％;N,N-二丙基-N’-对甲氧基苯磺酰脒（3c）对HCT116抑制率为80％,具有较好的抗肿瘤活性.

英文摘要：

Eleven sulfonyl amidine derivatives （3a ～ 3k） were synthesized by ＂one-pot＂ using tertiaryamines as the substrate,sulfonyl azides as nitrogen source and CuC1 as the catalyst.The structures were characterized by 1H NMR,13C NMR and HR-ESI-MS.3c,3e ～ 3i and 3k were new compounds.The in vitro antitumor activities of 3a ～ 3k were tested by MTT method.The results showed that 3a ～ 3k exhibited better antitumor activities agast A549,HCT116 and HepG220 cells at 20 μg ·mL-1.The inhibition of N,N-dipropyl-N＇-tosylformimidamide （3b） against A549 cells was 82 %,and N＇ [（4-methoxyphenyl） sulfonyl]-N,N-dipropylformimidamide （3c） against HCT116 cells was 80 %.