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T3P-assisted esterification and amidation of phosphinic acids
Authors:Erzsé  bet Jablonkai,Ré  ka Henyecz,Má  tyá  s Milen,Já  nos Kó  ti,Gyö  rgy Keglevich
Affiliation:1. Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, 1521 Budapest, Hungary;2. API Research and Development, Spectroscopic Research, Gedeon Richter Plc., 1475 Budapest, Hungary
Abstract:A few phosphinic acids, such as phenylphosphinic acids, 1-hydroxy-3-phospholene 1-oxides and 1-hydroxyphospholane oxides are esterified with simple alcohols in the presence of propylphosphonic anhydride (T3P®). If 1.1 equiv of the T3P® reagent is used, the esterifications are fast and efficient at 25° C. In the case of more reactive models it was enough to apply 0.66 equiv of T3P® at 85° C under microwave conditions. The amidation of 1-hydroxy-3-methyl-3-phospholene oxide could also be accomplished under similar conditions.
Keywords:Phosphinic acid   Phosphinic amide   P-Heterocycles   Phosphinate   T3P®   reagent   Green synthesis
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