Abstract:For the purpose of studying the structure-activity relationship of α-(substituted aniline)alkylphosphonate derivatives, a series of novel α-(substituted aniline)alkylphosphonates (1) was synthesized with substituted aniline and substituted benzaldehydes as starting materials reacting with dimethyl phosphite catalyzed by magnesium perchlorate. Compounds 1 reacted with t-Bu-NH2 to gain 2-methylpropan-2-aminium O-alkyl α-(substituted aniline)alkylphosphonate (2). The structures of compounds 2 were confirmed by 1H NMR, 13C NMR, IR, MS and elemental analyses. Preliminary bioassay results indicated that most of the title compounds exhibited good fungicidal activities, and exhibited better inhibition activities against tested fungi than that against bacteria. Compounds 2b and 2f displayed more than 75% inhibition against Phytophthora infestans at 500 ppm, which was slightly lower than that of dimethomorph.