Nitrogen-containing compounds are ubiquitously found in the fields of organic chemistry,pharmaceuticals,agrochemicals,medicinal chemistry and functional materials.The C-H bond amination reaction is one of the most str...Nitrogen-containing compounds are ubiquitously found in the fields of organic chemistry,pharmaceuticals,agrochemicals,medicinal chemistry and functional materials.The C-H bond amination reaction is one of the most straightforward protocols in the CN bond formation,showing"step"and"atomic"economy.As a catalyst for C-H amination reaction,copper exhibits its unique catalytic properties due to easily accessible oxidation states.The research progress of copper-catalyzed C-H amination in recent years is summarized.At the same time,reaction mechanisms are also briefly described in representative aminations to provide insights for the development prospects of highly practical and more environmentally benignprocesses.展开更多
Two series of thieno[2,3-d]pyrimidine derivatives were designed and synthesized, in which bioactive α-aminophosphonate subunits were introduced at the N3 position through an N-N bond connection. The in vitro cytotoxi...Two series of thieno[2,3-d]pyrimidine derivatives were designed and synthesized, in which bioactive α-aminophosphonate subunits were introduced at the N3 position through an N-N bond connection. The in vitro cytotoxic activity of the novel compounds was tested against human esophageal carcinoma cells （EC109）, human hepatocarcinoma cells （HepG2）, human gastric carcinoma cells （MGC-803）, respectively, by the MTT method. The evaluation results revealed that compounds fimb, 6mf, 6mg, 6rid and 6nh exerted the most potent inhibition against HepG2, MGC-803 and EC109 cells, respectively. In particular, compound 6rag presented excellent inhibitory effect against HepG2 （91.2%） and MGC-803 （94.4%） cells.展开更多
基金We are grateful for financial support from the National Natural Science Foundation of China(Nos.21938001,21961160741,22078072)the Special Innovation Project of Guangdong Provincial Department of Education(No.2021KTSCX082)+2 种基金the Science and Technology Plan Project of Maoming City(Nos.2020581,2021009,2021012)the Guangdong Basic and Applied Basic Research Foundation(No.2019A1515110346)the Scientific Research Foundation of Guangdong University of Petrochemical Technology(Nos.517152,2019rc053).
文摘Nitrogen-containing compounds are ubiquitously found in the fields of organic chemistry,pharmaceuticals,agrochemicals,medicinal chemistry and functional materials.The C-H bond amination reaction is one of the most straightforward protocols in the CN bond formation,showing"step"and"atomic"economy.As a catalyst for C-H amination reaction,copper exhibits its unique catalytic properties due to easily accessible oxidation states.The research progress of copper-catalyzed C-H amination in recent years is summarized.At the same time,reaction mechanisms are also briefly described in representative aminations to provide insights for the development prospects of highly practical and more environmentally benignprocesses.
基金supported by the National Natural Sciences Foundations of China (Nos.21171149,21105091)
文摘Two series of thieno[2,3-d]pyrimidine derivatives were designed and synthesized, in which bioactive α-aminophosphonate subunits were introduced at the N3 position through an N-N bond connection. The in vitro cytotoxic activity of the novel compounds was tested against human esophageal carcinoma cells （EC109）, human hepatocarcinoma cells （HepG2）, human gastric carcinoma cells （MGC-803）, respectively, by the MTT method. The evaluation results revealed that compounds fimb, 6mf, 6mg, 6rid and 6nh exerted the most potent inhibition against HepG2, MGC-803 and EC109 cells, respectively. In particular, compound 6rag presented excellent inhibitory effect against HepG2 （91.2%） and MGC-803 （94.4%） cells.
