A practical synthesis of α-aminophosphonic acids.
作者:J.P. Genêt、J. Uziel、M. Port、A.M. Touzin、S. Roland、S. Thorimbert、S. Tanier
DOI:10.1016/s0040-4039(00)77677-5
日期:1992.1
The preparation of diterbutyl-N (diphenylmethylene) aminomethylphosphonate 3 in four steps (42% overall yield) from N-hydroxymethyl phtalimide 1 is described. Various alpha-substituted alpha-aminophosphonic acids 5 containing functionalized unsaturated chains have been synthesized by alkylation of 3 under phase transfer catalysis with halides, Michael acceptors and palladium promoted reactions, followed by mild hydrolysis.