摘要 |
PROBLEM TO BE SOLVED: To obtain a new nitromethylsulfonamide derivative capable of exhibiting excellent aldose reductase-inhibiting action and preventing and treating effect of diabetic complication. SOLUTION: This nitromethylsulfonamide derivative is represented by formula I (A is an aryl or heterocyclic group; and R1 is H or an alkyl) or its pharmaceutically permissible salt, e.g. nitromethylsulfonamide. The derivative of formula I can be synthesized by reacting the corresponding amine derivative with methanesulfonyl chloride in the presence of an organic base, reacting the resultant methylsulfonamide derivative of formula II with an alkyl nitrate in the presence of a strong base and as necessary, further, reacting the reaction product with a base or an acid. The derivative of formula I is included as an active ingredient to provide the objective preventing or therapeutic agent for diabetic complication, which can prevent and treat, e.g. diabetic cataract, diabetic retinopathy, diabetic corneopathies, diabetic nephropathy, etc.
|