| 摘要 |
<p>NEW MATERIAL:A compound (acid addition salt) shown by the formula I [A is H, or (S)-4-amino-2-hydroxybutyryl]. EXAMPLE:5,2',3',4',4'',6''-Tetradeoxykanamycin. USE:A chemotherapeutic agent. A chemotherapeutic agent especially effective for various kinds of resistant bacteria. PROCESS:Four amino groups of a 3',4'-dideoxykanamycin shown by the formula II(R is H) are protected with amino-protecting groupa, this compound is treated with a base such as sodium hydroxide, etc. in an anhydrous aqueous solution, to give a compound shown by the formula III (R is amino-protecting group; R<1> and R<2> are OH). Hydroxyl groups at 2', 4'', and 6'' positions of this compound are sulfonated and thiophenylated, and hydrolyzed to give a deoxy compound shown by the formula III wherein R<1> is H. Hydroxyl group at 5 position of this compound is converted into S-methylthiocarbonyl group, and successively hydrolyzed, to give a 5-deoxy compound, and two amino-protecting groups are eliminated.</p> |
