Han Chun-min
2015
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Journal
Fine chemicals
Abstract
(S)-1-(2-Chloroacetyl) pyrrolidine-2-carbonitrile was synthesized from L-proline via successive reactions with chloro-acetyl chloride,ammoniated by 1,1'-carbonyldiimidazole with ammonium bicarbonate and dehydrated by phosphorus oxychloride;3-aminoadamantanol was synthesized from 1-adamantanamine hydrochloride which was previously nitrified by mixed acids,and then was replaced by alkali.This intermediate reacted with(S)-1-(2-chloroacetyl) pyrrolidine-2-carbonitrile to produce the target compound vildagliptin.The entire route is characterized by simple and easy access to raw materials,fewer steps,facile operation,and mild reaction conditions.The total yield of vildagliptin was increased from 32% to 42%,with a purity of more than 99%.The structure of product was characterized by means of IR,1HNMR and MS.