Synthesis and Activity Evaluation of Imidazolidinetrionylsaccharin Derivatives

1-Methyl-3-(1,1,3-trioxo-1,3-dihydro-1λ$^6$-benzo[d]isothiazol-2-ylmethyl)-imidazolidine-2,4,5-triones 5a, 1-ethy1-3-(1,1,3-trioxo-1,3-dihydro-lλ$^6$/-benzo[d]isothiazol-2-ylmethyl)-imidazolidine-2,4,5-triones 5b 1-phenyl-3-(1,1,3-trioxo-1,3-dihydro-1λ$^6$-benzo [d]isothiazol-2-ylmethyl)-imidazolidine-2,4,5-triones 5c were obtained by means of 4 reaction steps involved the reaction of 1-methyl-urea and oxalyl chloride. Biological tests(Plant Response Screening Result, Insect Primary Screening Result and Fungicide Primary Screening Result) of synthesized sacccarin derivatives were executed.

Imidazolidinetrionylsaccharin 유도체의 합성 및 활성평가

새로운 농약을 창출하기 위해, thiazole 유도체 등에서 살균력이 존재하는 구조를 가진 1,2-benzisothiazole-3-one-1,1-dioxide를 선도물질로 imidazolidinetrionyl 기를 가진 새로운 화합물을 합성하였다. 1-methylurea와 oxalyl chloride의 반응으로부터 4단계 반응을 거쳐 1-methyl-3-(1,1,3-trioxo-1,3-dihydro-1λ$^6$-benzo[d]isothiazol-2-ylmethyl) -imidazolidine-2,4,5-triones 5a, 1-ethyl-3- (1,1,3-trioxo-1,3-dihydro-1λ$^6$-benzo[d] isothiazo1-2-ylmethyl)-imidazolidine-2,4,5-triones 5b, 1-phenyl-3-(1,1,3- trioxo-1,3-dihydro-1λ$^6$-benzo[d]isothiazol-2-ylmethyl)-imidazolidine-2,4,5-triones 5c를 합성하였다. 합성된 5a, 5b, 5c를 식물반응, 곤충 그리고 살균제 등에 대한 생물학적 반응검색을 하였다. 생물학적 반응검색 결과(식물반응 검색은 5b, 곤충검색은 5a, 그리고 살균제 검색은 5a에서 생물활성이 조금 나타남) 썩 좋은 반응결과를 얻지 못했다. 하지만 계속해서 2,4,5-imidazolidinetrionyl기를 가진 saccharin유도체를 합성하여 새로운 농약을 창출하고자 한다.