21-SUBSTITUTED THIOSTEROID COMPOUND

NEW MATERIAL:A compound expressed by formula I (R and R are H or 1-6C alkyl; R is H, acetyl, 1-6C alkyl, 2-5C alkoxycarbonyl or 1-3C alkylthio; X is H or halogen; the dotted line, as necessary, indicates double bond). EXAMPLE:Desonide 21-thioacetate. USE:An anti-inflammatory gent, capable of being l...

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Bibliographische Detailangaben
Hauptverfasser:	SODA KAORU, MIKUCHI MORIKIMI, TAGUCHI MINORU, IKEMOTO TOMOYUKI, HATAYAMA KATSUO
Format:	Patent
Sprache:	eng
Schlagworte:	CHEMISTRY HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS STEROIDS
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Beschreibung
Zusammenfassung:	NEW MATERIAL:A compound expressed by formula I (R and R are H or 1-6C alkyl; R is H, acetyl, 1-6C alkyl, 2-5C alkoxycarbonyl or 1-3C alkylthio; X is H or halogen; the dotted line, as necessary, indicates double bond). EXAMPLE:Desonide 21-thioacetate. USE:An anti-inflammatory gent, capable of being locally administered, having powerful action and useful for treating various dermatoses, asthmas, allergic diseases and rheumatic diseases. PREPARATION:For example, a 21-sulfonyloxy steroid expressed by formula II is reacted with S-thioacetic acid, preferably at 1:1-3 molar ratio of the former to the latter in the presence of a base (e.g. sodium methoxide) in a solvent, such as acetone, preferably at 0-60 deg.C to afford the aimed compound expressed by formula III (R is acetyl).