Cyanoalkyl a-ring procursors

专利名称：Cyanoalkyl a-ring procursors发明人：COHEN; NOAL,ROSENBERGER;

MICHAEL,SAUCY; GABRIEL

申请号：US45070974申请日：19740313公开号：US3925420A公开日：19751209

摘要：A multi-step, stereospecific total synthesis of steroids utilizing intermediateshaving a cyanoalkyl A-ring precursor is disclosed. The initial starting materials for thisprocess are the relatively inexpensive and commercially available reagents lambda -butyrolactone and sodium cyanide. The process is suitable for the preparation of racemicor optically active, medicinally valuable steroids, particularly 19-norsteroids. It is afeature of this process that conditions employed during the multiple step synthesis areselected so as to retain the normally labile nitrile group even during hydrogenation andhydrolysis steps. In this manner, it is possible to employ the nitrile group as an A-ringprecursor without resorting to protective groups as was heretofore found necessary inprevious steroid total synthesis processes.

申请人：HOFFMANN-LA ROCHE INC.

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