abstract |
Steroids comprising 17-spirolactone or the corresponding open lactone structure are obtained by carbonylation of 17-alkenyl or 17-alkynyl substrates. 17-alkenyl intermediates may be prepared by semi-hydrogenation of 17-alkynyl groups. A number of schemes for the preparation of 3-keto-9,11-epoxy-17-spirolactone steroids such as eplerenone are disclosed. Preparation of such new intermediates or conversion of them to further intermediates or products, as well as new intermediates, by semi-hydrogenation, carbonylation, 6,7-dehydrogenation, purylation or other transformations or combinations thereof The step of making it is also disclosed. |