Designing Synthesis And Bioactivities Of α-Aminophosphonates Containing 3,4,5-Trimethoxyphenyl

Nine compounds were synthesized by the Mannich-type addition of O,O'-di-alkylphosphite to 3, 4, 5-trimethoxy benzaldehyde and 2-aminobenzothiazole was carried out in one pot at 100°C for 120 min solvent free and catalyst free condition. which is economic, conveniencent, high yields and environment-friendly. Their structures were clearly established by elemental analysis, IR, ¹H NMR and ¹³C NMR spectra. Single crystals of la have been obtained and determined. The crystalsystem of compound la belongs to monocline with space group P2(1)/c, a = 1.1212(2) nm, b = 1.6571(3) nm, c = 1.4689(3) nm,α= 90°,β=104°,γ= 90°, Z = 4, V= 2.6474(10) nm³, Dc = 1.314 mg/m³,μ=0.227 mm^-1, F(000) =1108 There exists an intramolecular hydrogen bond (N(2)-H(2)...O(2)) in the molecule of la.The results of bioassay show that compound 1e exhibits higher antiviral activity against tobacco mosaic virus (42.9%) at 500μg/mL than Ninnan meisu (40.6%), the other compounds showed moderate anti-tobacco mosaic virus (TMV) activity.