| 摘要 |
<p>NEW MATERIAL:The aprosamine derivative of formulaI(n is 0 or 1; the wavy line represents the axial of equatorial configuration), and its acid addition salt. EXAMPLE:3-Amino-2-hydroxypropyl beta-aprosaminide. USE:Antibacterial agent, bactericide, and disinfectant. It has strong antibacterial activity against Gram-positive and Gram-negative bacteria. PROCESS:The compound of formulaIis prepared by (1) protecting the 1, 3, 2' and 7'-position amino groups of aprosamine obtained by the hydrolysis of apramycin of formula II, (2) protecting the 5 and 6-position hydroxyl groups and acylating the 8'-position hydroxyl group of the product to obtain the compound of formula III, (3) subjecting the compound to intramolecular condensation reaction between the 6'-position hydroxyl group and the 7'-position amino group in the presence of a base, (4) carrying out the interchange of the 5- an 6-position protecting groups and the halogen-substitution of the 8'-position acyloxy group, (5) reacting the product with the compound of formula V, and (6) hydrolyzing the resultant compound of formula VI.</p> |
