发明名称 21-SUBSTITUTED THIOSTEROID COMPOUND
摘要 NEW MATERIAL:A compound expressed by formula I (R<1> and R<2> are H or 1-6C alkyl; R<3> 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<3> is acetyl).
申请公布号 JPS63215695(A) 申请公布日期 1988.09.08
申请号 JP19870047203 申请日期 1987.03.02
申请人 TAISHO PHARMACEUT CO LTD 发明人 MIKUCHI MORIKIMI;IKEMOTO TOMOYUKI;TAGUCHI MINORU;HATAYAMA KATSUO;SODA KAORU
分类号 A61K31/58;A61P29/00;C07J31/00;C07J71/00 主分类号 A61K31/58
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