应用化学
應用化學
응용화학
CHINESE JOURNAL OF APPLIED CHEMISTRY
2001年
2期
92-95
,共4页
哒嗪酮%氨基甲酸酯衍生物%合成%生物活性
噠嗪酮%氨基甲痠酯衍生物%閤成%生物活性
달진동%안기갑산지연생물%합성%생물활성
从2-取代-4.5-二氯哒嗪酮(1)出发,使2-取代-4-氯-5-羟基哒嗪酮(2)与溴乙基氨基甲酸酯反应合成含哒嗪酮的氨基甲酸酯类化合物(5a,5b).将化合物1与乙醇胺反应制得2-取代-4-氯-5-(2-氨基乙氧)哒嗪酮(3),化合物3与氯甲酸酯反应得到5a~51.化合物3催化加氢生成2-取代-5-(2-氨基乙氧)哒嗪酮(4).化合物4与氯甲酸酯在-10~-5℃反应得到化合物(6a~6d),在0~15 C反应得到相应N,N-二甲酸酯化合物(7a,7b).探讨了中间体3与4的反应活性.生物活性测试结果表明其中一些化合物具有较好的杀菌活性.
從2-取代-4.5-二氯噠嗪酮(1)齣髮,使2-取代-4-氯-5-羥基噠嗪酮(2)與溴乙基氨基甲痠酯反應閤成含噠嗪酮的氨基甲痠酯類化閤物(5a,5b).將化閤物1與乙醇胺反應製得2-取代-4-氯-5-(2-氨基乙氧)噠嗪酮(3),化閤物3與氯甲痠酯反應得到5a~51.化閤物3催化加氫生成2-取代-5-(2-氨基乙氧)噠嗪酮(4).化閤物4與氯甲痠酯在-10~-5℃反應得到化閤物(6a~6d),在0~15 C反應得到相應N,N-二甲痠酯化閤物(7a,7b).探討瞭中間體3與4的反應活性.生物活性測試結果錶明其中一些化閤物具有較好的殺菌活性.
종2-취대-4.5-이록달진동(1)출발,사2-취대-4-록-5-간기달진동(2)여추을기안기갑산지반응합성함달진동적안기갑산지류화합물(5a,5b).장화합물1여을순알반응제득2-취대-4-록-5-(2-안기을양)달진동(3),화합물3여록갑산지반응득도5a~51.화합물3최화가경생성2-취대-5-(2-안기을양)달진동(4).화합물4여록갑산지재-10~-5℃반응득도화합물(6a~6d),재0~15 C반응득도상응N,N-이갑산지화합물(7a,7b).탐토료중간체3여4적반응활성.생물활성측시결과표명기중일사화합물구유교호적살균활성.
Pyridazinone-carbamate derivatives 5a~51 were synthesized starting from 2-substituted4,5-dichloro pyridazinones 1 via two routes. One is that 2-substituted-4-chloro-5-hydroxyl pyridazinones 2 reacted with β-bromoethyl carbamates to afford compounds 5a and 5b. The other is that 2-substituted-4-chloro-5-(2-amino ethyloxyl)pyridazinones 3 obtained from the reaction of 1 with amino ethanol, reacted with chloroformate to give 5a~51. Furthermore, the catalytic hydrogenation of 3 gave 2-substituted-5-(2-amino ethyloxyl)pyridazinones 4, which reacted with chloromates to produce compounds 6a~6d at temperatures between -10~-5 C, and to N,N-dicarbamates 7a and 7b at 0~15 C. The reactivity of intermidiates 3 and 4 was also discussed. The preliminary bioassay indicated that almost all of the compounds showed fungicidal activities.