化学研究与应用
化學研究與應用
화학연구여응용
Chemical Research and Application
2015年
10期
1531-1538
,共8页
曾荣今%刘传磊%沈鹏飞%唐沙%熊春刚%吴湘思
曾榮今%劉傳磊%瀋鵬飛%唐沙%熊春剛%吳湘思
증영금%류전뢰%침붕비%당사%웅춘강%오상사
N1,N3-二烷基取代%3,4-二氢嘧啶-2(1H)-酮%无溶剂%相转移催化%抗菌活性
N1,N3-二烷基取代%3,4-二氫嘧啶-2(1H)-酮%無溶劑%相轉移催化%抗菌活性
N1,N3-이완기취대%3,4-이경밀정-2(1H)-동%무용제%상전이최화%항균활성
N1,N3-dialkylation%3,4-dihydropyrimidine-2(1H)-ones%solvent-free%phase transfer catalysis%fungicidal activity
在温和的相转移催化剂存在下,合成得到一系列N1,N3-二烷基取代-3,4-二氢嘧啶-2(1H)-酮,并测定了取代二氢嘧啶酮对灰霉菌、小麦赤霉菌、辣椒疫霉病菌、油菜菌核病菌、水稻纹枯病菌、稻瘟病菌六种霉菌的抗菌活性。多数取代二氢嘧啶酮对后五种霉菌体现出不错的抗菌活性,特别是N原子上被( CH2) n Br取代的二烷基取代二氢嘧啶酮对于油菜菌核病菌、小麦赤霉菌以及辣椒疫霉病菌表现出不错的抗菌活性。数据表明,二氢嘧啶酮中嘧啶环和酯基上的取代基变化有助于改善嘧啶酮的抗菌活性。
在溫和的相轉移催化劑存在下,閤成得到一繫列N1,N3-二烷基取代-3,4-二氫嘧啶-2(1H)-酮,併測定瞭取代二氫嘧啶酮對灰黴菌、小麥赤黴菌、辣椒疫黴病菌、油菜菌覈病菌、水稻紋枯病菌、稻瘟病菌六種黴菌的抗菌活性。多數取代二氫嘧啶酮對後五種黴菌體現齣不錯的抗菌活性,特彆是N原子上被( CH2) n Br取代的二烷基取代二氫嘧啶酮對于油菜菌覈病菌、小麥赤黴菌以及辣椒疫黴病菌錶現齣不錯的抗菌活性。數據錶明,二氫嘧啶酮中嘧啶環和酯基上的取代基變化有助于改善嘧啶酮的抗菌活性。
재온화적상전이최화제존재하,합성득도일계렬N1,N3-이완기취대-3,4-이경밀정-2(1H)-동,병측정료취대이경밀정동대회매균、소맥적매균、랄초역매병균、유채균핵병균、수도문고병균、도온병균륙충매균적항균활성。다수취대이경밀정동대후오충매균체현출불착적항균활성,특별시N원자상피( CH2) n Br취대적이완기취대이경밀정동대우유채균핵병균、소맥적매균이급랄초역매병균표현출불착적항균활성。수거표명,이경밀정동중밀정배화지기상적취대기변화유조우개선밀정동적항균활성。
A series of novel N1,N3-dialkylated 3,4-dihydropyrimidin-2(1H)-ones were synthesized under mild phase transfer cata-lyst( PTC) . Their fungicidal activities against Botrytis cinerea,Gibberella zeae,Phytophythora capsici,Sclerotinia sclerotiorum,Rhi-zoctonia solani and Pyricularia oryzae were investigated. Most of the N1,N3-dialkylated DHPMs 4 had high fungicidal activities a-gainst the five latter,especially the compounds with the substituents(R3=(CH2)nBr)exhibited excellent fungicidal activities a-gainst Sclerotinia sclerotiorum,Gibberella zeae and Phytophythora capsici. The studies of all the compounds revealed the advantages of substituents on the pyrimidine and the ester group( R2=CH2 CH3 and R3=( CH2 ) n Br) to the fungicidal activity.