| 摘要 |
<p>1446082 Kanamycin B derivatives ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI 21 Aug 1974 [29 Aug 1973] 36782/74 Heading C2C The invention comprises compounds selected from 1,21 - di - N - (4 - amino - 2 - hydroxybutyryl) - kanamycin B, 1,2<SP>1</SP> - di - N - (4 - amino- 2 - hydroxy butyryl) - 3<SP>1</SP>,4<SP>1</SP> - dideoxykanamycin B, 1,2<SP>1</SP> - di - N - isoseryl kanamycin B and 1,2<SP>1</SP> - di - N - isoseryl - 3<SP>1</SP>,4<SP>1</SP> - dideoxy kanamycin B, which are generically represented by a 1,2<SP>1</SP> - di - N - (α- hydroxy - aminoacyl)kanamycin B or -3<SP>1</SP>,4<SP>1</SP>-dideoxy kanamycin B of the general Formula I wherein R each is a hydroxyl group or each is a hydrogen atom and n is an integer of 1 or 2 and pharmaceutically acceptable acid-addition salts thereof. The compounds of Formula I may be prepared by acylating a compound of general formula wherein R each is a hydroxyl group or each is a hydrogen atom, and R 1 is a known mono-valent amino-protecting group and R 2 is a hydrogen atom, or R 1 and R 2 taken together form a known divalent amino protecting group, with anα-hydroxy amino acid of the formula wherein R 3 is a known mono-valent aminoprotecting group and R 4 is a hydrogen atom, or R 3 and R 4 taken together form a known divalent amino-protecting group, and n is an integer of 1 or 2, to produce the mixed N-acylated products containing the desired intermediate acylation product of the formula removing the amino protecting groups from said mixed N acylated products and then isolating the desired compound out of the mixed N- acylated products which have been freed from the amino-protecting groups. The compounds of Formula I are used as antibiotics.</p> |
