二氟甲基取代吡唑甲酰胺类化合物的合成及杀菌活性

Synthesis and fungicidal activity of difloromethyl-1H- pyrazole-4-carboxamides

摘要: 以二氟乙酰乙酸乙酯和原甲酸三乙酯为起始原料,经亲核取代、环化、水解、氯代和酰化反应得到N-(1-甲基-2-羟乙基)-3-二氟甲基-1-甲基-1 H -吡唑-4-酰胺(4),4与取代异氰酸酯作用,合成了10个未见文献报道的二氟甲基取代吡唑甲酰胺类衍生物,其结构均经过1H NMR和MS分析确证。初步生物活性测试结果表明,在50 mg/L下,目标化合物 ZJ-3、ZJ-5、ZJ-7、ZJ-8 对瓜类炭疽病菌、瓜类灰霉病菌和水稻纹枯病菌具有一定的杀菌活性。

Abstract: Ten novel difluoromethyl substituted pyrazolecarboxamide derivatives were synthesized with nucleophilic substitution,cyclization,hydrolysis,esterification and addition reaction using ethyl 4,4-difluoro-3-oxobutanoate and triethoxymethane as raw materials.Their structures were confirmed by 1H NMR and MS.The preliminary bioassay showed that target compounds ZJ-3,ZJ-5,ZJ-7 and ZJ-8 exhibit some inhibiting effects against Gibberella zeae,Botrytis cinerea and Rhizoctonia solani at the concentration of 50 mg/L.