| 摘要 |
<p>PURPOSE:To obtain industrially advantageously an acid addition salt of antibiotic dactimicin having antibacterial actions on various kinds of Gram-negative and Gram-positive bacteria, by using a derivative of fortimicin B or fortimicin A as a starting material. CONSTITUTION:A fortimicin B derivative shown by the formula I (R' is a protecting group removable by hydrolysis under acidic conditions) is reacted with a glycine derivative shown by the formula II (R<2> is a protecting group removal by decomposition through hydrogenation; Z is an active group of carboxylic acid) to give a compound shown by the formula III, which is subjected to decomposition through dehydrogenation, so that the protecting group R<2> is removed to give a compound shown by the formula IV. This compund shown by the formula IV is reacted with a compound shown by the foumula V (R<3> is 1-4C alkyl; HX is HCl, HBr, etc.) to form a compound shown by the formula VI, which is hydrolyzed with an acid(e.g., CF3CO2H), so that the protecting group R<1> is removed to give an acid addtion salt of a compound shown by the formula VII (a saft of the acid used, e.g., CF3CO2H, HCl, etc.), and if necessary, the acid addition salt is converted into another acid addtion salt.</p> |
