| 摘要 |
<p>NEW MATERIAL:Compounds of formula I [R is H, alpha-hydroxy-omega-aminoalkanoly of formula II (n is 1, 2)]. EXAMPLE:3',4'-Dideoxykanamycin A of formula III. USE:Antibiotic for curing microbism containing diseases caused by resistant bacteria. PREPARATION:For example, a protecting derivative of kanamycin A of formula IV (A is 1-4C alkylsulfonyl; B is 2-5C alkoxycarbonyl; Y is 1-6C alkylidene) is treated with sodium hydride in an organic solvent to form a 4', 6'-cyclic carbamate. The product is made to react with an acetal in the presence of an acidic catalyst to give the 2'5'-O-protecting derivative and then the carbamate ring is cleaved and then acetylated. The product is subjected to O-sulfonylation and treatment with potassium iodide to give 3'-eno form derivative, hydrogenation and finally the protecting group for amino group is removed by a usual method to give the objective compound.</p> |
