Rational synthesis of α-hydroxyphosphonic derivatives including dronic acids

Abstract

New, green methods have been elaborated for the syntheses of α-hydroxyphosphonates and α-hydroxymethylenebisphosphonic derivatives (HMBPs, dronates). α-Hydroxyphosphonates were prepared via the Pudovik reaction, while the synthesis of HMBPs has been performed in the three-component reaction of carboxylic acids, phosphorus trichloride and phosphorus acid.

Graphical Abstract

Keywords:

• α-Hydroxymethylenebisphosphonates
• α-hydroxyphosphonates
• Pudovik reaction
• green syntheses
• sulfolane
• ionic liquid

Additional information

Funding

The above project was supported by the National Research Development and Innovation Fund (K119202). Z. Rádai is grateful for the fellowship provided by Chinoin–Sanofi Pharmaceuticals and József Varga Foundation. Z. Rádai was supported by the ÚNKP-18-3-IV-BME-265 New National Excellence Program of the Ministry of Human Capacities.