Compounds of the formula
wherein
A is =0, α-H:β-OH or α-OH:β-H;
R1 is H or a blocking group; and
R3 is H, C1.8 alkyl, C1.4 mono-, di- or tri-haloalkyl,
-R31-O-R32or -R31-NR33R34 in which R31 is C1-4 alkylene, R32 is H or C1-6 alkyl, R33 is H or C, a alkyl and R34 is H, C1-6 alkyl or a blocking group, provided that the number of carbon atoms in R31 and R32, in R31 and R33 and in R31 and R34 (if R34 is alkyl) is not more than 7; and pharmacologically acceptable salts thereof.
These sugar-ring expanded analogues of spectinomycin and its C-6' derivatives are prepared from 7-membered sugar-ring spectinomycin and spectinomycin derivatives, by treatment with sodium borohydride.
式中的化合物
式中
A 是 =0、α-H:β-OH 或 α-OH:β-H;
R1 是 H 或封端基团;以及
R3 是 H、C1.8 烷基、C1.4 单卤烷基、二卤烷基或三卤烷基、
-R31-O-
R32or-R31-NR33R34,其中 R31 为 C1-4 亚烷基,
R32 为 H 或 C1-6 烷基,R33 为 H 或 C,a 烷基,R34 为 H、C1-6 烷基或封端基团,条件是 R31 和
R32、R31 和 R33 以及 R31 和 R34(如果 R34 为烷基)中的碳原子数不超过 7;及其药理学上可接受的盐。
光谱霉素及其 C-6' 衍
生物的这些糖环扩展类似物是用
硼氢化钠处理 7 元糖环光谱霉素和光谱霉素衍
生物制备的。