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Patent / Jan 01, 1971

Mineral hydroxy acid esters of 9.alpha.-fluoro-16-methylprednisolone

  • Ivan Villax
US 3564028

Prepn. of the title compds., useful for the remission of pain, bleeding tendency, and fever, is described. Orthophosphoric acid (85%) is dehydrated; MeCN and Et3N added and the mixt. cooled to and ClCO2Et in MeCN added. The mixt. is stirred 0.5 hr followed by the addn. of prednisolone in MeCN and Et3N. The mixt. is refluxed 1 hr, and 2N NaOMe in MeOH added to yield Na salt of prednisolone 21-phosphate, m. Similarly are prepd. 6 addnl. analogs.