Inflazyme Pharmaceuticals Ltd.

Gueijun Ji

David L Burgoyne

Yaping Shen

Yuanlin Zhou

Nicholas D Paschalides

Eugene W Kelleher

Kishore Ramachandran

Steroids containing a cyclohexene moiety are efficiently oxidized to the corresponding &#x3b1;,&#x3b2;-unsaturated ketone using copper iodide and t-butyl hydroperoxide. A steroid compound containing the &#x3b1;,&#x3b2;-unsaturated ketone structure is efficiently converted to the corresponding vicinal diol using a hydroborating reagent followed by oxidative workup, e.g., borane followed by sodium perborate. Benzoyl and substituted benzoyls are superior protecting groups for hydroxyl groups present in the compounds.

Process improvements in steroid chemistry

Steroids containing a cyclohexene moiety are efficiently oxidized to the corresponding &agr;,&bgr;-unsaturated ketone using copper iodide and t-butyl hydroperoxide. A steroid compound containing the &agr;,&bgr;-unsaturated ketone structure is efficiently converted to the corresponding vicinal diol using a hydroborating reagent followed by oxidative workup, e.g., borane followed by sodium perborate. Benzoyl and substituted benzoyls are superior protecting groups for hydroxyl groups present in the compounds.

Process for the production of 6,7-diols of steroidal compounds

Growing community of inventors

Richmond, CA, United States of America

Gueijun Ji