A series of novel 3,5-dichloro-4-（1,1,2,2-tetrafluoroethoxy）phenyl containing 4-methyl-l,2,3-thiadiazole derivatives were designed and synthesized via Ugi reaction. Their structures were confirmed by IR, 1H NMR, 13C...A series of novel 3,5-dichloro-4-（1,1,2,2-tetrafluoroethoxy）phenyl containing 4-methyl-l,2,3-thiadiazole derivatives were designed and synthesized via Ugi reaction. Their structures were confirmed by IR, 1H NMR, 13C NMR and high-resolution mass spectroscopy. The preliminary bioassay results indicated that some title compounds had good fungicide activity at 50 ug/mL; most of the compounds presented a certain degree of direct inhibition activity, good inactivation and curative activity against tobacco mosaic virus at 500 ug/mL and 100 ug/mL; some compounds showed good larvicidal activity against Plutella xylostella L. at 200 ug/mL and excellent larvicidal activities against Culex pipiens pallens at 2 ug/mL.展开更多
The first total synthesis of talaroconvolutin A(1.1 g obtained)and talarofuranone has been achieved using accessible materials(12 steps,7.5%and 8.2%yields,respectively).Convergent routes involved intramolecular Diels-...The first total synthesis of talaroconvolutin A(1.1 g obtained)and talarofuranone has been achieved using accessible materials(12 steps,7.5%and 8.2%yields,respectively).Convergent routes involved intramolecular Diels-Alder reactions in two approaches for creating the decalin moiety.Additionally,an unprecedented DMP-mediated domino reaction resulted in the deoxy-tetramic acid system.These syntheses not only establish the absolute configuration of talaroconvolutin A but also enable further collaborative studies of this typeofferroptosisinducers.展开更多
This paper describes a concise and practical route to enantiomerically enriched 5-alkyl substituted nicotine analogs. The Vilsmeier reaction was used to construct the nicotinaldehydes ring followed by the introduction...This paper describes a concise and practical route to enantiomerically enriched 5-alkyl substituted nicotine analogs. The Vilsmeier reaction was used to construct the nicotinaldehydes ring followed by the introduction of the chiral homoallylic alcohol by organic boron reagent and the cyclization of the pyrrolidine ring through the reduction of a chiral azide. 17 analogs have been synthesized and their corresponding biological activities were tested, in which compounds 10d and 10g exhibit excellent ICs0 values against RD and SY-SY5Y.展开更多
The easily accesible azidoethylacetate 1 was reacted with ferrocene formaldehyde to give azide 2, which was allowed to take Staudinger reactions with triphenylphosphine to give iminophosphorane 3. The imidazolinone de...The easily accesible azidoethylacetate 1 was reacted with ferrocene formaldehyde to give azide 2, which was allowed to take Staudinger reactions with triphenylphosphine to give iminophosphorane 3. The imidazolinone derivatives containing ferrocenyl moity(5a～5e) were synthesized by a tandem aza-Wittig reaction of 3 with phenyl isocynate and substituted phenols in yields of 57%～69%. The structures of title compounds were confirmed by elemental analysis,IR and 1H NMR. Two of them 5b and 5c exhibited fungicidal activities and none of them has herbicidal activity and insecticidal activity.展开更多
基金Project supported by the National Natural Science Foundation of China （Nos. 20872071, 20911120069）, the Tianjin Natural Science Foundation （No. 10JCZDJC17500）, the National Key Project for Basic Research （No. 2010CB126105）, the National Key Technology Research and Development Program （Nos. 2011BAE06B02, 2011BAE06B05） and the Foundation of Achievements Transformation and Spreading of Tianjin Agricultural Science and Technology （No. 201002250）, the Russian Foundation for Basic Research （Nos. RFBR 08-03-00376 a and RFBR/NNSF 08-03-92208 a）.
文摘A series of novel 3,5-dichloro-4-（1,1,2,2-tetrafluoroethoxy）phenyl containing 4-methyl-l,2,3-thiadiazole derivatives were designed and synthesized via Ugi reaction. Their structures were confirmed by IR, 1H NMR, 13C NMR and high-resolution mass spectroscopy. The preliminary bioassay results indicated that some title compounds had good fungicide activity at 50 ug/mL; most of the compounds presented a certain degree of direct inhibition activity, good inactivation and curative activity against tobacco mosaic virus at 500 ug/mL and 100 ug/mL; some compounds showed good larvicidal activity against Plutella xylostella L. at 200 ug/mL and excellent larvicidal activities against Culex pipiens pallens at 2 ug/mL.
基金This work was supported by the National Natural Science Foundation of China(Nos.82073714 and 32271539)the National Key Research and Development Program of China(No.2023YFF1104001)Fundamental Research Funds for the Central Universities,South-Central Minzu University(No.CZY23025).
文摘The first total synthesis of talaroconvolutin A(1.1 g obtained)and talarofuranone has been achieved using accessible materials(12 steps,7.5%and 8.2%yields,respectively).Convergent routes involved intramolecular Diels-Alder reactions in two approaches for creating the decalin moiety.Additionally,an unprecedented DMP-mediated domino reaction resulted in the deoxy-tetramic acid system.These syntheses not only establish the absolute configuration of talaroconvolutin A but also enable further collaborative studies of this typeofferroptosisinducers.
文摘This paper describes a concise and practical route to enantiomerically enriched 5-alkyl substituted nicotine analogs. The Vilsmeier reaction was used to construct the nicotinaldehydes ring followed by the introduction of the chiral homoallylic alcohol by organic boron reagent and the cyclization of the pyrrolidine ring through the reduction of a chiral azide. 17 analogs have been synthesized and their corresponding biological activities were tested, in which compounds 10d and 10g exhibit excellent ICs0 values against RD and SY-SY5Y.
文摘The easily accesible azidoethylacetate 1 was reacted with ferrocene formaldehyde to give azide 2, which was allowed to take Staudinger reactions with triphenylphosphine to give iminophosphorane 3. The imidazolinone derivatives containing ferrocenyl moity(5a～5e) were synthesized by a tandem aza-Wittig reaction of 3 with phenyl isocynate and substituted phenols in yields of 57%～69%. The structures of title compounds were confirmed by elemental analysis,IR and 1H NMR. Two of them 5b and 5c exhibited fungicidal activities and none of them has herbicidal activity and insecticidal activity.
