Process for preparing phosphonous acids

Details Process for preparing phosphonous acids Process for preparing phosphonous acids

1987-01-20

1988-04-26

Evans, J. E.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

2605025D, 560130, C07F 948

Patent

active

047403322

ABSTRACT:
A process is provided for preparing phosphonous acids of the structure wherein R.sub.1 is lower alkyl or arylalkyl ##STR1## which are useful in preparing phosphinic and phosphonic acid ACE inhibitors, which process includes the steps of treating an olefin of the structure R.sub.1 --CH.dbd.CH.sub.2 wherein R.sub.2 is lower alkyl or arylalkyl with a phosphorus-containing reagent such as sodium hypophosphite or hypophosphorous acid in the presence of an organic alcohol solvent such as ethanol or methanol, and a radical initiator such as azobisisobutyronitrile, under acidic conditions, preferably at the reflux temperature of the organic solvent, to form the phosphonous acid without forming the alkyl ester.

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deBataafsche, "Production of Phosphonous Acid Derivatives", Chem. Abst. 8145c, 46 (1952).
Smith, "Intramolecular Esters of Hydroxy or Amino Phosphinic Acids", Chem. Abst., 8252d, 48 (1954).

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