Trialkysilyl trifluoromethanesulfonate mediated functionalization of 4-aza-5alpha-androstan-3-one steroids.

摘要

A novel single-pot trialkylsilyl trifluoromethanesulfonate (R3Si-OTf) mediated process produces derivatives of 4-aza 3-keto steroids at the alpha -methylenic carbon through electrophilic substitution. These derivatives are useful in the preparation, through elimination of the substituent on the alpha -methylene carbon, of DELTA -l olefin 4-aza 3-keto steroids which are potent inhibitors of 5- alpha reductase.