发明名称 NOVEL PREPARATION OF 1-EPIAMINOGLUCOSIDE
摘要 <p>PURPOSE:To obtain the titled compound useful as an antimicrobial agent and a synthetic intermediate therefor in high yield, by oxidizing a specific aminoglucoside with a peroxide in the presence of a specified metallic catalyst, and reducing the resultant oxidation product electrolytically to epimerize the NH2 group at the 1- position. CONSTITUTION:The functional group other than the NH2 group at the 1-position of a compound expressed by formula I (R<1> is OH or NH2;R<2>,R<3> and R<6> are H or OH; R<4> is CH2NH2, CH2OH, etc.; R<5> is NH2 or ethylamino; R<7> is OH or CH3; R<8> is H, CH2OH, etc.) is protected if necessary. The compound is then oxidized with a peroxide in the presence of a catalyst containing a metal of Group Vb or VIb in the periodic talble to give a compound of formula III (A is group of formula V; B is group of formula VI; X is protecting group of the amino group), which is then reduced electrolytically to afford the compound of formula IV. The protecting group of the comound expressed by formula IV is then removed if necessary to give a 1- epiaminoglucoside of formula II.</p>
申请公布号 JPS56138198(A) 申请公布日期 1981.10.28
申请号 JP19800040595 申请日期 1980.03.28
申请人 SHIONOGI SEIYAKU KK 发明人 IGARASHI KIKUO;SUGAWARA TAMIO;HONMA TSUNETOSHI
分类号 C07H15/234;C07H15/22 主分类号 C07H15/234
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