发明名称 21-SUBSTITUTED THIOSTEROID COMPOUND
摘要 NEW MATERIAL:A compound expressed by formula I (R<1> is 2-6C alkanoyl or methylthioacetyl; R<2> is H, acetonyl, 2-propynyl, 2-5C alkoxycarbonyl, etc.; R<3> is H or methyl; X is H or halogen; Y is H or methyl; the bond between the 1- and the 2-positions may be double bond). EXAMPLE:21-Deoxyhydrocortisone 17alpha-butyrate 21-thiol. USE:An anti-inflammatory agent. PREPARATION:For example, a 21-acetylthiosteroid expressed by formula II is hydrolyzed with a base, such as hydrazine, in tetrahydrofuran at -20-+5 deg.C temperature to provide a compound expressed by formula III, which is then reacted with an acetonyl halide, etc., in the presence of a base to afford the aimed compound expressed by formula I.
申请公布号 JPS63303994(A) 申请公布日期 1988.12.12
申请号 JP19870138978 申请日期 1987.06.04
申请人 TAISHO PHARMACEUT CO LTD 发明人 MIKUCHI MORIKIMI;IKEMOTO TOMOYUKI;TAGUCHI MINORU;HATAYAMA KATSUO;SODA KAORU
分类号 A61K31/57;A61P29/00;C07J31/00 主分类号 A61K31/57
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