| 摘要 |
<p>NEW MATERIAL:An XK-62-4 derivative of formula I: (n is 1, 2, or 3) or its acid addition salt. EXAMPLE:1-N-(alpha-Hydroxy-beta-aminopropionyl)XK-62-4. USE:Antibiotics having antibacterial activities against Gram-positive and Gram- negative bacteria, particularly Escherichia coli resistant to aminoglycoside antibiotics. PROCESS:The amino group at the 2'-position of the XK-62-4 of formula II is protected by an amino-protecting agent in a solvent, e.g. tetrahydrofuran, at -50 to 50 deg.C to give a compound of formula III: (Y1 is H; Y2 is group of formula IV, etc.), which is concentrated and acylated with an acylating agent to form a compound of formula V: (Y3 is H; Y4 is group of formula IV, etc.), which is concentrated. The protecting group is eliminated by the well-known method to afford the compound of formula I.</p> |
