Trialkylsilyl trifluoromethanesulfonate mediated alpha -methylenic carbon functionalization of 4-aza-5 alpha -androstan-3-one steroids

Trialkylsilyl trifluoromethanesulfonate mediated alpha -methylenic carbon functionalization of 4-aza-5 alpha -androstan-3-one steroids

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 alph...

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Bibliographische Detailangaben
Hauptverfasser: SHUMAN, RICHARD F, ANDERSON, KEVIN, ABRAMSON, NEWTON L, KARADY, SANDOR, DOUGLAS, ALAN W, KING, ANTHONY O
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
STEROIDS
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Zusammenfassung: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 -1 olefin 4-aza 3-keto steroids which are potent inhibitors of 5- alpha reductase.