Dihydro-(2H)-1 .2.4-benzothiadizine-1. 1-dioixdes were prepared in good yields via reductive cyclization of o-nitrobenzenesulfonamidcs with aldchydes promoted by Sml2 under mild and neutral condition.
H 1,2,4 Benzothiadiazine 1,1 dioxide derivatives have been widely used in pharmaceutical chemistry.The formation of thiazide ring is a key step for preparing these compounds.Here we described a novel synthesis of the ...H 1,2,4 Benzothiadiazine 1,1 dioxide derivatives have been widely used in pharmaceutical chemistry.The formation of thiazide ring is a key step for preparing these compounds.Here we described a novel synthesis of the titled compounds in which the thiazide ring is formed conveniently by employing phosphorus oxychloride as dehydrating agent.The structures of the products were characterized by means of elemental analysis, 1HNMR,IR and ultraviolet spectra etc.The total yields of the titled compounds are above 45 percent.展开更多
To discover novel strobilurins analogues with good and broad spectrum activity,a series of nove 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides-based strobilurins was designed,synthesized,and tested agains various ...To discover novel strobilurins analogues with good and broad spectrum activity,a series of nove 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides-based strobilurins was designed,synthesized,and tested agains various phytopathogenic fungi.Compounds 7b.7c.and 7k exhibited substantial and broad spectrum antifungal activities against the tested phytopathogenic fungi,especially compound 7b,which showed 100%,80%,90%,and 90%antifungal activity(in virto)against Erysiphe graminis(E.graminis),Puccinia sorghi Schw:(P sorghi Schw.)Colletotrichum lagenarium(C.lagenarium),and Pseudoperonospora cubensis(P cubensis)at 300 ug/mL,respectively.better or comparable to the positive control azoxystrobin.Moreover,compound 7b exhibited 85%greenhouse inhibi.tion activity(in vivo)against E.graminis even at 0.2μg/mL,equal to azoxystrobin(90%)and trifloxystrobin(90%)Meanwhile,compound 7b against P cubensis displayed 70%and 55%greenhouse inhibition activity(in vivo)at 1.56 and 0.2μg/mL,respectively,much better than those of azoxystrobin and trifloxystrobin(both 0%at 1.56 and 0.2 ug/mL).Therefore,compound 7b could be considered as the most promising fungicidal candidate for furthe study.Furthermore,based on the effective concentration(ECso)against C.arachidicola,the built CoMSIA model provided the useful reference for the further structural optimization design.展开更多
文摘Dihydro-(2H)-1 .2.4-benzothiadizine-1. 1-dioixdes were prepared in good yields via reductive cyclization of o-nitrobenzenesulfonamidcs with aldchydes promoted by Sml2 under mild and neutral condition.
文摘H 1,2,4 Benzothiadiazine 1,1 dioxide derivatives have been widely used in pharmaceutical chemistry.The formation of thiazide ring is a key step for preparing these compounds.Here we described a novel synthesis of the titled compounds in which the thiazide ring is formed conveniently by employing phosphorus oxychloride as dehydrating agent.The structures of the products were characterized by means of elemental analysis, 1HNMR,IR and ultraviolet spectra etc.The total yields of the titled compounds are above 45 percent.
基金Supported by the Scientific Project of Tianin Municipal Education Commission,China(No.2018KJ008).
文摘To discover novel strobilurins analogues with good and broad spectrum activity,a series of nove 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides-based strobilurins was designed,synthesized,and tested agains various phytopathogenic fungi.Compounds 7b.7c.and 7k exhibited substantial and broad spectrum antifungal activities against the tested phytopathogenic fungi,especially compound 7b,which showed 100%,80%,90%,and 90%antifungal activity(in virto)against Erysiphe graminis(E.graminis),Puccinia sorghi Schw:(P sorghi Schw.)Colletotrichum lagenarium(C.lagenarium),and Pseudoperonospora cubensis(P cubensis)at 300 ug/mL,respectively.better or comparable to the positive control azoxystrobin.Moreover,compound 7b exhibited 85%greenhouse inhibi.tion activity(in vivo)against E.graminis even at 0.2μg/mL,equal to azoxystrobin(90%)and trifloxystrobin(90%)Meanwhile,compound 7b against P cubensis displayed 70%and 55%greenhouse inhibition activity(in vivo)at 1.56 and 0.2μg/mL,respectively,much better than those of azoxystrobin and trifloxystrobin(both 0%at 1.56 and 0.2 ug/mL).Therefore,compound 7b could be considered as the most promising fungicidal candidate for furthe study.Furthermore,based on the effective concentration(ECso)against C.arachidicola,the built CoMSIA model provided the useful reference for the further structural optimization design.
