The target compound, ethyl 2-(3-(4-fluorobenzamido)phenyl)-4-((4-fluorobenzoyl)oxy) thiazole-5-carboxylate, was synthesized by four-step procedures including N-protection, thionation, cyclization and acylation...The target compound, ethyl 2-(3-(4-fluorobenzamido)phenyl)-4-((4-fluorobenzoyl)oxy) thiazole-5-carboxylate, was synthesized by four-step procedures including N-protection, thionation, cyclization and acylation. Its structure was characterized by 1 H NMR, 13C NMR, HRMS and single-crystal X-ray diffraction. The target compound crystallizes as monoclinic crystal system, space group C2/c with a = 9.6097(19), b = 14.246(3), c = 33.070(7) ?, V = 4515.1(16) ?3, Z = 8, Dc = 1.496 Mg/m3, F(000) = 2096 and μ = 0.203 mm-1. There are 21864 reflections measured(4.94≤2θ≤55.96°), of which 5357 were unique(Rint = 0.1418) and used in all calculations. The final R = 0.0581(I > 2σ(I)) and wR = 0.1453(reflections). The target compound showed over 50% of growth inhibition against Physalospora piricola, Rhizoctonia cerealis and Sclerotinia sclerotiorum.展开更多
基金supported in part by the International Science&Technology Cooperation Program of China(2014DFR41030)the Tianjin Natural Science Foundation(18JCZDJC33500)the National Natural Science Foundation of China(31571991,31872007)
文摘The target compound, ethyl 2-(3-(4-fluorobenzamido)phenyl)-4-((4-fluorobenzoyl)oxy) thiazole-5-carboxylate, was synthesized by four-step procedures including N-protection, thionation, cyclization and acylation. Its structure was characterized by 1 H NMR, 13C NMR, HRMS and single-crystal X-ray diffraction. The target compound crystallizes as monoclinic crystal system, space group C2/c with a = 9.6097(19), b = 14.246(3), c = 33.070(7) ?, V = 4515.1(16) ?3, Z = 8, Dc = 1.496 Mg/m3, F(000) = 2096 and μ = 0.203 mm-1. There are 21864 reflections measured(4.94≤2θ≤55.96°), of which 5357 were unique(Rint = 0.1418) and used in all calculations. The final R = 0.0581(I > 2σ(I)) and wR = 0.1453(reflections). The target compound showed over 50% of growth inhibition against Physalospora piricola, Rhizoctonia cerealis and Sclerotinia sclerotiorum.