Entity

Time filter

Source Type


Jin W.,Henan Agricultural University | Xie G.,Henan Agricultural University | Xie G.,Henan Provincial Key Laboratory of the Discovery and Application of Novel Pesticide | Sun S.,Henan Agricultural University | And 8 more authors.
Chinese Journal of Organic Chemistry | Year: 2014

A new procedure for synthesizing 4,5-dimethyl-2-(trimethylsilyl)thiophene-3-carboxamide derivatives was explored. Using commercially available 3-mercaptobutan-2-one and methyl propiolate as starting materials, the target compounds were obtained in four steps via silylanization of methyl propiolate, cyclization, selective hydrolysis and amidation. And the promoters involved in silylanization, cyclization and selective hydrolysis were screened. The procedure exhibited several advantages such as easily available raw materials, mild reaction conditions, easily purified intermediates and high single-step yields. It had potential to be applied to scale production. © 2014 Chinese Chemical Society & SIOC, CAS. Source


Xie G.,Henan Agricultural University | Xie G.,Henan Provincial Key Laboratory of the Discovery and Application of Novel Pesticide | Jin W.,Henan Agricultural University | Zhao Y.,Henan Agricultural University | And 10 more authors.
Chinese Journal of Organic Chemistry | Year: 2014

The procedures for synthesizing the substituted ester 2-hydrothiophene-3-carboxylate and its silanization were explored. The reaction conditions were optimized. And with the substituted thiophene as the framework, 20 new thiophene carboxamide derivatives were synthesized. The chemical structures of thiophene carboxamide derivatives were confirmed by 1H NMR, 13C NMR, HRMS or elemental analysis techniques. The inhibitory activity against Gaeumannomyces graminis var. tritici was evaluated in vitro by the plate method. The preliminary structure-activity relationship indicated that the substituent bonded to the amide nitrogen atom and the steric hindrance of the substituent at 2nd position of the thiophene carboxamide had a significant influence on the activity. The compounds 7b~7d, 7l, 7m and 7o exhibited very high inhibitory activity. The results would be helpful for the design of lead compounds. © 2014 Chinese Chemical Society & SIOC, CAS. Source

Discover hidden collaborations