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3-Amino-1-adamantanol is an important adamantane drug intermediate mainly used in the synthesis of inhibitors with antihyperglycaemic properties for the preparation of Vildagliptin, a dipeptidyl peptidase 4 (DPP-4) inhibitor used in the treatment of type 2 diabetes.

White solid

3-Amino-1-hydroxyadamantane can be employed in the synthesis of inhibitors with antihyperglycemic properties.

As reagent, 3-Amino-1-hydroxyadamantane can be used in the preparation of Vildagliptin.

A preparation method of 3-amino-1-adamantanol comprises the following steps: (1) adding amantadine or a salt thereof to sulfuric acid at 10-30 DEG C and adding a mixed acid dropwise to perform a nitration reaction to obtain a reaction liquid; (2) adding the reaction liquid to water and mixing the reaction liquid with water to obtain a mixed solution; (3) performing a hydroxylation reaction under the effect of alkaline to obtain the 3-amino-1-adamantanol. The preparation method employs the raw material, is easy to obtain, is simple in operations, is environmentally protective, is low in cost, and is high in yield, which is generally higher than 80%, maximally 90.1%.

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