Microwave assisted efficient Hantzsch reaction via four-component coupling reactions of tetrazolo[1,5-α]quinoline-4-carbal-dehyde, dimedone/cyclohexane-1,3-dione,ethyl/methyl acetoacetate and ammonium acetate was des...Microwave assisted efficient Hantzsch reaction via four-component coupling reactions of tetrazolo[1,5-α]quinoline-4-carbal-dehyde, dimedone/cyclohexane-1,3-dione,ethyl/methyl acetoacetate and ammonium acetate was described as the preparation of tetrazolo[1,5-α]quinoline based 1,4-dihydropyridines,acridine-1,8-diones and polyhydroquinolines.The process presented here is simple,rapid,environmentally welcoming and high yielding.All the derivatives were subjected to an in vitro antimicrobial screening against a representative panel of bacteria and fungi and results worth further investigations.展开更多
A series of 10-methyl-1,2,3,4,5,6,7,8,9,10-decahydroacridine-1,8-dione derivatives were synthesized by one-pot reaction of aldehyde, dimedone or 1,3-cyclohexanedione and methylamine in glycol or water under microwave ...A series of 10-methyl-1,2,3,4,5,6,7,8,9,10-decahydroacridine-1,8-dione derivatives were synthesized by one-pot reaction of aldehyde, dimedone or 1,3-cyclohexanedione and methylamine in glycol or water under microwave heating without catalyst. The method has the advantage of short routine and reaction time, high yields as well as friendly environment. And the reaction was not only suitable for aliphatic and aromatic monoaldehyde, but also for aromatic dialdehyde.展开更多
Benzo[1,2-b:4,5-b′]dithiophene(BDT) has been widely used to construct donor-acceptor(D-A) copolymers in organic solar cells(OSCs). However, benzo[1,2-b:4,5-b′]difuran(BDF), an analogue of BDT, has received less atte...Benzo[1,2-b:4,5-b′]dithiophene(BDT) has been widely used to construct donor-acceptor(D-A) copolymers in organic solar cells(OSCs). However, benzo[1,2-b:4,5-b′]difuran(BDF), an analogue of BDT, has received less attention than BDT. The photovoltaic performance of BDF copolymers has lagged behind that of BDT copolymers. Here, we designed and synthesized two BDF copolymers, PBF1-C and PBF1-C-2Cl. PBF1-C-2Cl, which is composed of BDF and benzo[1,2-c:4,5-c′]dithiophene-4,8-dione connected by a chlorinated thiophene π-bridge, displays a low-lying highest occupied molecular orbital energy level,which helps in yielding a high open-circuit voltage(Voc) in OSCs. As a result, when blended with Y6, PBF1-C-2Cl-based devices showed a high Voc of 0.83 V and a power conversion efficiency(PCE) of 13.10%. To the best of our knowledge, the PCE of 13.10% is among the highest efficiency values for OSCs based on BDF copolymers.展开更多
Based on the hit 5-hydroxy-2-methyl-10-propyl-2,3-dihydro-4H,8H-pyrano[2,3-j]chromene-4,8-dione（1）, a series of pyrano[2,3-f]chromene-4,8-dione derivatives was designed and synthesized using pb_loroghicinol as start...Based on the hit 5-hydroxy-2-methyl-10-propyl-2,3-dihydro-4H,8H-pyrano[2,3-j]chromene-4,8-dione（1）, a series of pyrano[2,3-f]chromene-4,8-dione derivatives was designed and synthesized using pb_loroghicinol as startingmaterial. Meanwhile, a regioselective synthetic route was developed for 5-methoxy-2,3-dihydro-4H,8H-pyrano-[2,3-f]chromene-4,8-dione products（11a-11f）, and their structures were further confirmed by nuclear Overhausereffect（NOE）. The evaluation of anticancer activities of these compounds against four human cancer cell lines,including human glioma cell line （SHG-44）, human lung cancer cell line（H1299）, breast cancer cell line（/vICF7） andhuman colon carcinoma cell line（HCT-116） in vitro shows that 5-methoxy-2,2-dimethyl-9-chloro-10-trifluormethyl-2,3-dihydro-4H,8H-pyrano[2,3-f]chromene-4,8-dione（lle） possesses the best anticancer activities with IC50 values of6.68, 7.90, 5.16 and 4.82 gmol/L, respectively. Finally, the preliminary structure-activity relationships（SARs） weresttmmarized, which could pave the way for generating more potent anticancer agents with drug-like properties.展开更多
文摘Microwave assisted efficient Hantzsch reaction via four-component coupling reactions of tetrazolo[1,5-α]quinoline-4-carbal-dehyde, dimedone/cyclohexane-1,3-dione,ethyl/methyl acetoacetate and ammonium acetate was described as the preparation of tetrazolo[1,5-α]quinoline based 1,4-dihydropyridines,acridine-1,8-diones and polyhydroquinolines.The process presented here is simple,rapid,environmentally welcoming and high yielding.All the derivatives were subjected to an in vitro antimicrobial screening against a representative panel of bacteria and fungi and results worth further investigations.
基金Project supported by the National Natural Science Foundation of China （No. 20372057） and the Natural Science Foundation of Jiangsu Province （No. BK2001142）.
文摘A series of 10-methyl-1,2,3,4,5,6,7,8,9,10-decahydroacridine-1,8-dione derivatives were synthesized by one-pot reaction of aldehyde, dimedone or 1,3-cyclohexanedione and methylamine in glycol or water under microwave heating without catalyst. The method has the advantage of short routine and reaction time, high yields as well as friendly environment. And the reaction was not only suitable for aliphatic and aromatic monoaldehyde, but also for aromatic dialdehyde.
基金supported by the National Natural Science Foundation of China (21674007, 51825301, 21975012, 21875204, 21875204, 21734001)the financial support from the National Research Foundation (NRF) of Korea (NRF-2019R1A2C2085290, 2019R1A6A1A11044070).
文摘Benzo[1,2-b:4,5-b′]dithiophene(BDT) has been widely used to construct donor-acceptor(D-A) copolymers in organic solar cells(OSCs). However, benzo[1,2-b:4,5-b′]difuran(BDF), an analogue of BDT, has received less attention than BDT. The photovoltaic performance of BDF copolymers has lagged behind that of BDT copolymers. Here, we designed and synthesized two BDF copolymers, PBF1-C and PBF1-C-2Cl. PBF1-C-2Cl, which is composed of BDF and benzo[1,2-c:4,5-c′]dithiophene-4,8-dione connected by a chlorinated thiophene π-bridge, displays a low-lying highest occupied molecular orbital energy level,which helps in yielding a high open-circuit voltage(Voc) in OSCs. As a result, when blended with Y6, PBF1-C-2Cl-based devices showed a high Voc of 0.83 V and a power conversion efficiency(PCE) of 13.10%. To the best of our knowledge, the PCE of 13.10% is among the highest efficiency values for OSCs based on BDF copolymers.
文摘Based on the hit 5-hydroxy-2-methyl-10-propyl-2,3-dihydro-4H,8H-pyrano[2,3-j]chromene-4,8-dione（1）, a series of pyrano[2,3-f]chromene-4,8-dione derivatives was designed and synthesized using pb_loroghicinol as startingmaterial. Meanwhile, a regioselective synthetic route was developed for 5-methoxy-2,3-dihydro-4H,8H-pyrano-[2,3-f]chromene-4,8-dione products（11a-11f）, and their structures were further confirmed by nuclear Overhausereffect（NOE）. The evaluation of anticancer activities of these compounds against four human cancer cell lines,including human glioma cell line （SHG-44）, human lung cancer cell line（H1299）, breast cancer cell line（/vICF7） andhuman colon carcinoma cell line（HCT-116） in vitro shows that 5-methoxy-2,2-dimethyl-9-chloro-10-trifluormethyl-2,3-dihydro-4H,8H-pyrano[2,3-f]chromene-4,8-dione（lle） possesses the best anticancer activities with IC50 values of6.68, 7.90, 5.16 and 4.82 gmol/L, respectively. Finally, the preliminary structure-activity relationships（SARs） weresttmmarized, which could pave the way for generating more potent anticancer agents with drug-like properties.
