synthesis and bioactivity of a-aminophosphonates containing fluorinea-aminophosphonates含有氟原子的合成和生物活性.pdf

Molecules 2003, 8, 186– 192 molecules ISSN 1420-3049 Synthesis and Bioactivity of a-Aminophosphonates Containing Fluorine Bao-An Song *, Yang -Lan Wu, Song Yang, De-Yu Hu, Xiang -Qiong He and Lin-Hong Jin Research and Development Center of Fine Chemicals, Guizhou University, Guiyang, 550025, P.R. China * Author to whom correspondence should be addressed; E-mail: gzgdjh@ Abstract: Twenty-one a-aminophosphonates containing fluorine were synthesized by Mannich-type reactions. Their structures were established by elemental analysis, IR, 1H- NMR and MS. In field tests, some of these new compounds display high antiviral activity against the tobacco mosaic virus (TMV). The molecular geometry of compound 4f was determined by X-ray diffraction structure analysis. Keywords: a-Aminophosphonates, synthesis, bioactivity Introduction It is known that a -aminophosphonic acids and their derivatives display interesting bioactivities such as antiphytoviral, antitumor, herbicidal and fungicidal activity, therefore they have attracted considerable attention in pesticide and medicine formulation. A large volume of research on their synthesis and biological activities has been reported during the last twenty years [1-8], but little attention has been paid to the synthesis of a-aminophosphonates bearing fluorine. Considering that fluorine has special biomimetic, electronegativity, blocking and lipophilic effects, once introduced into organic compounds, there may be profound and unexpected