Triethyl phosphite → Diethyl 4-cyano-2-fluorobenzylphosphonate

Participants

Reaction Conditions

Reaction Steps

A mixture of 4-(bromomethyl)-3-fluorobenzonitrile (1.5 g, 7.0 mmol)[J. Med. Chem., 40, 2064 (1997)] and triethyl phosphite (1.4 g, 8.4 mmol) was heated at 150° C. for 2 hours. At the end of this time, the reaction mixture was concentrated under reduced pressure. Volatile materials in the residue thus obtained were removed by heating said residue at 100° C. in vacuo for 1 hour to afford the title compound (1.97 g, quantitative yield) as an oil which solidified in the freezer. This oily product was used in the next step without further purification.

Provenance & Evidence