Asymmetric Synthesis of Aminophosphonic Acids and Trifluoromethylated Derivatives Thereof

Abstract

Various approaches leading to chiral aminophosphonic acids were described. Catalytic asymmetric-induced addition of dialkylphosphite to chiral aldimine gives low ee. value. The diastereoselective alkylation of bicyclic phosphonamide derived from anilinomethylpyrrolidine and followed by subsequent reactions provide much better results. 1,3-Proton Schiff reaction was applied successfully for chiral trifluoromethylated f - and/or g -aminophosphonic acids.

Keywords:

• Aminophosphonic Acids
• Asymmetric Synthesis
• 1,3-PSR
• Trifluoromethylated Derivatives