Eighteen 2′,4′-difluoro-3-(carbamoyl)biphenyl-4-yl benzoates were synthesized from diflunisal in three steps with total yields from 72% to 86%. All compounds were identified by IR, 1^H NMR, MS and elemental analys...Eighteen 2′,4′-difluoro-3-(carbamoyl)biphenyl-4-yl benzoates were synthesized from diflunisal in three steps with total yields from 72% to 86%. All compounds were identified by IR, 1^H NMR, MS and elemental analysis. The anti-inflammatory activity and analgesic activity for 18 compounds were evaluated. The preliminary assay results showed that compounds 4a and 4p exhibited potent anti-inflammatory-analgesic activity.展开更多
In the presence of In/CuCl, ethyl 4-bromo-4,4-difluoro-3-oxo-2-(triphenylphosphoranylidene)butanoate reacted with various aldehydes in aqueous medium at room temperature to give the a,a-difluorinated β-hydroxy carb...In the presence of In/CuCl, ethyl 4-bromo-4,4-difluoro-3-oxo-2-(triphenylphosphoranylidene)butanoate reacted with various aldehydes in aqueous medium at room temperature to give the a,a-difluorinated β-hydroxy carbonyl compounds. Furthermore, treating Reformatsky addition compounds with 1 equiv, of sodium hydroxide in the mixture of tetrahydrofuran and water afforded gem-difluoromethylenated 2-triphenylphosphoranylidene δ-lactones in excellent yields.展开更多
A pH-sensor with a pKa value of 5.05 based on 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene(BODIPY) dye was synthesized and demonstrated to be highly sensitive within a pH range of 4.0--6.0 and was highly photostable, ...A pH-sensor with a pKa value of 5.05 based on 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene(BODIPY) dye was synthesized and demonstrated to be highly sensitive within a pH range of 4.0--6.0 and was highly photostable, which makes it a potential pH fluorescent probe. The new pH-sensor will find its application in studying acidic organelles in living cells.展开更多
Three novel symmetrical 4.4'-difluoro-4-bora-3a,4a-diaza-sindacene(BODIPY) derivatives were synthesized via a general and efficient protocol. These BODIPY dyads bear a diverse aryl linker bridge in the middle and t...Three novel symmetrical 4.4'-difluoro-4-bora-3a,4a-diaza-sindacene(BODIPY) derivatives were synthesized via a general and efficient protocol. These BODIPY dyads bear a diverse aryl linker bridge in the middle and two BODIPY units at the termini. The photophysical properties of these dyads were investigated by ultravioletvisible(UV-Vis) absorption and emission spectroscopy. And their electrochemical properties were studied by cyclic voltammetry. The absorption of these dyads showed slightly blue shift and the intramolecular charge transfer(ICT) state under,vent ultrafast direct surface crossing to the ground state with high degree of rotational freedom. The results will be useful for the further functionalization of these novel symmetrical BODIPY derivatives.展开更多
基金the Opening Foundation of The Biochemical Engineering Key Discipline (No.20050105) Zhejiang,China,for financial supportthe National Center for Drug Screening,Shanghai,China,for evaluation of anti-inflammatory and analgesic activity.
文摘Eighteen 2′,4′-difluoro-3-(carbamoyl)biphenyl-4-yl benzoates were synthesized from diflunisal in three steps with total yields from 72% to 86%. All compounds were identified by IR, 1^H NMR, MS and elemental analysis. The anti-inflammatory activity and analgesic activity for 18 compounds were evaluated. The preliminary assay results showed that compounds 4a and 4p exhibited potent anti-inflammatory-analgesic activity.
基金Project supported by the National Natural Science Foundation of China (NNSFC) (Nos. 20972050, 21172148).
文摘In the presence of In/CuCl, ethyl 4-bromo-4,4-difluoro-3-oxo-2-(triphenylphosphoranylidene)butanoate reacted with various aldehydes in aqueous medium at room temperature to give the a,a-difluorinated β-hydroxy carbonyl compounds. Furthermore, treating Reformatsky addition compounds with 1 equiv, of sodium hydroxide in the mixture of tetrahydrofuran and water afforded gem-difluoromethylenated 2-triphenylphosphoranylidene δ-lactones in excellent yields.
基金Supported by the State Basic Research Project of China(No.2002CB713808)
文摘A pH-sensor with a pKa value of 5.05 based on 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene(BODIPY) dye was synthesized and demonstrated to be highly sensitive within a pH range of 4.0--6.0 and was highly photostable, which makes it a potential pH fluorescent probe. The new pH-sensor will find its application in studying acidic organelles in living cells.
基金the National Natural Science Foundation of China
文摘Three novel symmetrical 4.4'-difluoro-4-bora-3a,4a-diaza-sindacene(BODIPY) derivatives were synthesized via a general and efficient protocol. These BODIPY dyads bear a diverse aryl linker bridge in the middle and two BODIPY units at the termini. The photophysical properties of these dyads were investigated by ultravioletvisible(UV-Vis) absorption and emission spectroscopy. And their electrochemical properties were studied by cyclic voltammetry. The absorption of these dyads showed slightly blue shift and the intramolecular charge transfer(ICT) state under,vent ultrafast direct surface crossing to the ground state with high degree of rotational freedom. The results will be useful for the further functionalization of these novel symmetrical BODIPY derivatives.