DI-EPOXIDE PROCESS FOR THE PREPARATION OF 9{60 -FLUORO-16-METHYLENE-PREDNISOLONE OR-PREDNISONE, AND 21-ESTERS THEREOF

DI-EPOXIDE PROCESS FOR THE PREPARATION OF 9{60 -FLUORO-16-METHYLENE-PREDNISOLONE OR-PREDNISONE, AND 21-ESTERS THEREOF

In the preparation of 9 alpha -fluoro-16-methylene-prednisolone or -prednisone and 21-esters thereof, 9 beta , 11 beta ; 16 alpha , 17 alpha -diepoxy-16 beta -methylprogesterone is reacted, in any desired sequence, with hydrogen fluoride and with a microbiological 1(2)-dehydrogenation agent, to prod...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: KLAUS IRMSCHER, DIETER ORTH
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
STEROIDS
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:In the preparation of 9 alpha -fluoro-16-methylene-prednisolone or -prednisone and 21-esters thereof, 9 beta , 11 beta ; 16 alpha , 17 alpha -diepoxy-16 beta -methylprogesterone is reacted, in any desired sequence, with hydrogen fluoride and with a microbiological 1(2)-dehydrogenation agent, to produce 9 alpha -fluoro-16-methylene-1,4-pregnadiene-11 beta ,17 alpha -diol-3,20-dione. The resultant compound is then subjected to acetoxylation at the 21-position. Thereafter, 9 alpha -fluoro-16-methyleneprednisolone-21-acetate is optionally converted to corresponding prednisone by treatment with an oxidizing agent, and/or the 21-acetoxy-group is saponified to form the corresponding 9 alpha -fluoro-16-methyleneprednisolone or -prednisone, and/or the free 21-OH groups are esterified.