摘要 |
<p>NEW MATERIAL:2-Deoxyfortimicin B of formula I or its salts. USE:Antibiotic, effective on gramm-positive and negative microorganisms. PREPARATION:In fortimicin B of formula II, all primary amines are protected with benzyloxycarbonyl groups and the hydroxyl group on the carbon in the 5-position and the secondary amino group on the carbon in the 4-position are protected by forming oxazolidine rings using an adequate aldehyde to form a compound of formula III. The resulting compound is treated with hydrocarbon sulfonyl halide or its anhydride to form the methanesulfonate ester, then the oxazolidine rings are hydrolyzed to obtain a compound of formula IV. The product is catalytically hydrogenated in the presence of an acid to remove the N-protecting groups, treated with an aion exchanging resin to prepare the compound of formula V as a free base. Finally, the compound is catalytically reduced to afford the compound of formula I.</p> |