N-Alkylated benzimidazole derivatives have been synthesized via the aza-Michael addition reactions of1H-benzimidazoles to a,b-unsaturated compounds in water and palladium acetate obviously promoted these transformatio...N-Alkylated benzimidazole derivatives have been synthesized via the aza-Michael addition reactions of1H-benzimidazoles to a,b-unsaturated compounds in water and palladium acetate obviously promoted these transformations. The reported method, overcoming the inactivation of palladium under the equivalent nitrogenous conditions, has the advantages of convenient manipulation, atom-economy, as well as environmental friendliness. The bioactive results showed that butyl 3-（5,6-dimethyl-1Hbenzo[d]imidazol-1-yl）propanoate（3c） exhibited excellent inhibitory activity against Bacillus subtilis（MIC = 16 mg/m L） and Bacillus proteus（MIC = 8 mg/m L）. Therefore, this process would facilitate the construction of various potential bioactive compounds based on the benzimidazole scaffold under mild conditions.展开更多
A series of novel bridged-neonicotinoid analogues were designed and synthesized, which were constructed by starting material 8 with cyclopentenone or cyclohexenone in the presence of catalyst aluminium chloride. All o...A series of novel bridged-neonicotinoid analogues were designed and synthesized, which were constructed by starting material 8 with cyclopentenone or cyclohexenone in the presence of catalyst aluminium chloride. All of the compounds were characterized and confirmed by^1H NMR,^（13）C NMR, HRMS and IR. The bioassay tests showed that compounds 5 and 6a showed higher bioactivities than imidacloprid against Aphis craccivora.展开更多
基金supported by the National Natural Science Foundation of China(Nos.21004075,21372186)Beijing National Laboratory of Molecular Sciences(BNLMS)(No.20140130)+1 种基金the Doctoral Fund of Southwest University(No.SWU111075)the Research Funds for the Central Universities(No.XDJK2013C112)
文摘N-Alkylated benzimidazole derivatives have been synthesized via the aza-Michael addition reactions of1H-benzimidazoles to a,b-unsaturated compounds in water and palladium acetate obviously promoted these transformations. The reported method, overcoming the inactivation of palladium under the equivalent nitrogenous conditions, has the advantages of convenient manipulation, atom-economy, as well as environmental friendliness. The bioactive results showed that butyl 3-（5,6-dimethyl-1Hbenzo[d]imidazol-1-yl）propanoate（3c） exhibited excellent inhibitory activity against Bacillus subtilis（MIC = 16 mg/m L） and Bacillus proteus（MIC = 8 mg/m L）. Therefore, this process would facilitate the construction of various potential bioactive compounds based on the benzimidazole scaffold under mild conditions.
基金financial supported by Shandong Provincial Natural Science Foundation (No. ZR2015BL009)The Key Research and Development Program of Shandong Provincial (No. 2016GGX107006)+1 种基金National Natural Science Foundation of China (No. 21501066)the Opening Project of Shanghai Key Laboratory of Chemical Biology
文摘A series of novel bridged-neonicotinoid analogues were designed and synthesized, which were constructed by starting material 8 with cyclopentenone or cyclohexenone in the presence of catalyst aluminium chloride. All of the compounds were characterized and confirmed by^1H NMR,^（13）C NMR, HRMS and IR. The bioassay tests showed that compounds 5 and 6a showed higher bioactivities than imidacloprid against Aphis craccivora.
