Industriale Chimica S.r.l.

Francesco Barbieri

Roberto Lenna

Maria Giovanna Luoni

Johannes Bernardus Maria Rewinkel

Riccardo Di Brisco

Monica Noseda

Daniele Giudici

A process for the synthesis of &#x3b2;-hydroxy 3-17-(1H-benzimidazol-1-yl)androsta-5,16-diene is described, a compound also known as Galeterone and used in the treatment of prostate cancer, having the formula (6). 

Process for the preparation of 3&#x3b2;-hydroxy-17-(1H-benzimidazol-1-YL) androsta-5,16-diene

A process is described wherein, by employing 17&#x3b1;-(3-hydroxypropyl)-6&#x3b2;,7&#x3b2;;15&#x3b2;,16&#x3b2;-dimethylene-5&#x3b2;-androstane-3&#x3b2;,5,17&#x3b2;-triol (II) as starting product, in a single stage reaction there is obtained drospirenone, (I), a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic action, that is useful for preparing pharmaceutical compositions with contraceptive action. 

Process for the preparation of drospirenone

An improved process for the preparation of intermediate (V) through the elimination of a molecule of water from intermediate (IV) is described. Intermediate (V) is a key molecule for the synthesis of eplerenone, a synthetic steroid with pharmacological activity used in the treatment of chronic pathological conditions, including hypertension.

Process for the preparation of 7 &#x3b1;-(methoxycarbonyl)-3-OXO-17alpha-pregn-4,9(11)-dien-21,17-carbolactone, a useful intermediate for the synthesis of molecules with pharmacological activity

A process is disclosed wherein, using either 17a-(3-hydroxypropyl)-6p,7p;15p,16p-dimethylene-5p-androstane-3p,5,17p-triol (II) or 3&#x3b2;,5^&#xef;I^&#x3ba;^-6&#x3b2;,7&#x3b2;;15&#x3b2;,16&#x3b2;-dimethylene-5&#x3b2;,17&#x3b1;-pregnane-21,17-carbolactone (III) as starting material, through a single-step reaction it is obtained drospirenone (I), a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action. 

A process is described, comprising the oxidation of 17&#x3b1;-(3-hydroxypropyl)-6&#x3b2;,7&#x3b2;,15&#x3b2;,16&#x3b2;-dimethylen-5&#x3b2;-androstan-3&#x3b2;,5,17&#x3b2;-triol, for the preparation of drospirenone, a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action.

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Bovisio Masciago, Italy

Francesco Barbieri