| 摘要 |
PROBLEM TO BE SOLVED: To obtain the subject new compound having a marked glycosidase inhibitory activity and useful as a diabetes mellitus-treating agent, etc. SOLUTION: This azepane derivative is a compound of the formula [R1 to R4 are each OH, H, azido or a (substituted) amino and 2-3 of them are each OH], e.g. (3R, 4R, 5R, 6R)-hexahydro-3-azido-4,5,6-trihydroxy-1H-azepine. The compound of the formula is obtained by e.g. using pyranose as a raw material, converting primary hydroxyl group at 6 position to p-toluenesulfonyloxy group, etc., effecting sodium azide, etc., on it to form 6-azido-6-deoxypyranose, then performing a reductive aminoalkylation reaction by using palladium-carbon, etc., to obtain a tetrahydroxyazepane derivative, blocking a cyclic amino group and a part of hydroxyl groups with appropriate blocking groups, then converting the residual hydroxyl groups to desired hydrogen atom, azido group or a (substituted) amino group and then removing the blocking groups.
|
