一锅法合成N1,N3-二烷基取代-3,4-二氢嘧啶-2（1H）-酮及其抗菌活性研究.pdfVIP

第27卷第10期 化 学 研 究 与 应 用 Vol.27,No.10 　第10期 龚爱琴,:表等面: 活性剂增敏荧光法测定血清及药物中度他雄胺 　 2015年10月 ChemicalResearchandApplication Oct. ,2015 文章编号:1004-1656(2015)10-1531-08 One-pot synthesis and fungicidal activity of N1,N3-dialkylated3,4-dihydropyrimidin-2(1H)-ones 1,2* 1,2 1,2,3 1,2 1,2 1,2 ZENG Rong-jin ,LIU Chuan-lei ,SHEN Peng-fei ,TANG Sha ,XIONG Chung-ang ,WU Xiang-si (1.School of Chemistry and Chemical Engineering,Hunan University of Science and Technology,Xiangtan411201,China; 2.Key Laboratory of Theoretical Chemistry and Function Molecule of Ministry of Education, Hunan University of Science and Technology,Xiangtan411201,China; 3.School of Chemistry and Chemical Engineering,Hunan Normal University,Changsha410012,China.) Abstract:A series of novelN1,N3-dialkylated3,4-dihydropyrimidin-2(1H)-oneswere synthesizedunder mildphasetransfer 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 theN1,N3-dialkylated DHPMs4 had high fungicidal activities a- gainst the five latter,especially the compounds with the substituents(R =(CH ) Br)exhibited excellent fungicidal activities a- 3 2 n gainst Sclerotiniasclerotiorum,GibberellazeaeandPhytophythoracapsici.The studiesof allthecompoundsrevealedtheadvantages of substituents on the pyrimidine and the ester group(R =CH CH and R =(CH ) Br)to thefungicidal activity. 2 2 3 3 2 n Ke