Abstract
Efficient and high yielding methods for the preparation of vildagliptin 1 intermediate of ( S )-1-(2-chloroacetyl) pyrrolidine-2-carbonitrile 2 and 3-amino-1-adamantane alcohol 3 respectively have been described. ( S )-1-(2-Chloroacetyl) pyrrolidine-2-carbonitrile 2 has been synthesized from l-proline 2a via chloroacetyl chloride, performed with acetonitrile in the presence of sulfuric acid via one-pot reactions. 3-Amino-1-adamantane alcohol 3 has been prepared from amantadine hydrochloride via oxidation by sulfuric acid/nitric acid and boric acid as catalyst, and has been subjected to ethanol extraction. The overall yield is about 95%.
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