Borylative cyclization of E-3-arylallyl carbamoyl chlorides is achieved through copper catalyzed intramolecular carboboration with B_(2)pin_(2).2-Aryl-3-boryl-γ-lactams are formed with exclusive cisdiastereoselectivi...Borylative cyclization of E-3-arylallyl carbamoyl chlorides is achieved through copper catalyzed intramolecular carboboration with B_(2)pin_(2).2-Aryl-3-boryl-γ-lactams are formed with exclusive cisdiastereoselectivity.CuBr-Dppp combination gives the best outcomes.The substrate scope is profiled.展开更多
A series of novel triazole derivatives containing y-lactam were designed and synthesized, and their structures were confirmed by IH NMR, 13C NMR and HRMS, The in vitro antifungal activities of the target compounds wer...A series of novel triazole derivatives containing y-lactam were designed and synthesized, and their structures were confirmed by IH NMR, 13C NMR and HRMS, The in vitro antifungal activities of the target compounds were evaluated, The results showed that all of the compounds exhibited stronger activity against the six clinically important fungi tested than fluconazole. 3D and 3E showed comparative activity against the fungi tested except for Candida glabrata and Aspergillus fumigatus as voriconazole. In addition, the docking model for 2A and CYP51 was investigated.展开更多
以N-乙酰-L苯丙氨酸为唯一碳源进行初筛,手性HPLC测酶活力进行复筛,从海泥、海水、土壤等环境中筛选到一株(+)γ-内酰胺降解菌BH24。经形态学、生理生化、16S r DNA序列分析鉴定及系统发育分析,菌株BH24鉴定为苏云金芽孢杆菌(Bacillus t...以N-乙酰-L苯丙氨酸为唯一碳源进行初筛,手性HPLC测酶活力进行复筛,从海泥、海水、土壤等环境中筛选到一株(+)γ-内酰胺降解菌BH24。经形态学、生理生化、16S r DNA序列分析鉴定及系统发育分析,菌株BH24鉴定为苏云金芽孢杆菌(Bacillus thuringiensis),为获取(+)γ-内酰胺酶提供了一种新的菌源。来源于菌株BH24的(+)γ-内酰胺酶,最适温度为28℃,最适p H值为7.0。展开更多
A simple and eco-friendly method for the preparation of 1,5-diaryl-3-（arylamino）-lH-pyrrol-2（5H）-ones via the cyclo-condensation reaction of aldehydes, amines and ethyl pyruvate in the presence of silica supported...A simple and eco-friendly method for the preparation of 1,5-diaryl-3-（arylamino）-lH-pyrrol-2（5H）-ones via the cyclo-condensation reaction of aldehydes, amines and ethyl pyruvate in the presence of silica supported ferric chlo- ride （SiO2-FeCl3） as reusable heterogeneous catalyst is described. The present methodology offers several advantages such as excellent yields, simple procedure and short reaction times.展开更多
基金the National Natural Science Foundation of China(No.21672027)for financial supportsupported by High-Level Entrepreneurial Talent Team of Jiangsu Province(No.2017-37)。
文摘Borylative cyclization of E-3-arylallyl carbamoyl chlorides is achieved through copper catalyzed intramolecular carboboration with B_(2)pin_(2).2-Aryl-3-boryl-γ-lactams are formed with exclusive cisdiastereoselectivity.CuBr-Dppp combination gives the best outcomes.The substrate scope is profiled.
基金supported by the National Natural Science Foundation of China (No. 21402223)
文摘A series of novel triazole derivatives containing y-lactam were designed and synthesized, and their structures were confirmed by IH NMR, 13C NMR and HRMS, The in vitro antifungal activities of the target compounds were evaluated, The results showed that all of the compounds exhibited stronger activity against the six clinically important fungi tested than fluconazole. 3D and 3E showed comparative activity against the fungi tested except for Candida glabrata and Aspergillus fumigatus as voriconazole. In addition, the docking model for 2A and CYP51 was investigated.
文摘以N-乙酰-L苯丙氨酸为唯一碳源进行初筛,手性HPLC测酶活力进行复筛,从海泥、海水、土壤等环境中筛选到一株(+)γ-内酰胺降解菌BH24。经形态学、生理生化、16S r DNA序列分析鉴定及系统发育分析,菌株BH24鉴定为苏云金芽孢杆菌(Bacillus thuringiensis),为获取(+)γ-内酰胺酶提供了一种新的菌源。来源于菌株BH24的(+)γ-内酰胺酶,最适温度为28℃,最适p H值为7.0。
文摘A simple and eco-friendly method for the preparation of 1,5-diaryl-3-（arylamino）-lH-pyrrol-2（5H）-ones via the cyclo-condensation reaction of aldehydes, amines and ethyl pyruvate in the presence of silica supported ferric chlo- ride （SiO2-FeCl3） as reusable heterogeneous catalyst is described. The present methodology offers several advantages such as excellent yields, simple procedure and short reaction times.
