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Title: An efficient synthesis of Vildagliptin intermediates
Authors: Li, Yufei
Jiang, Lan
Zhang, Li
Wang, Jingyu
Xiang, Peng
Pan, Junyi
Hu, Xiangnan
Keywords: Vildagliptin;intermediate;3-amino-1-adamantane alcohol;(S)-1-(2-chloroacetyl) pyrrolidine-2-carbonitrile
Issue Date: Aug-2021
Publisher: NIScPR-CSIR, India
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%.
Page(s): 1128-1131
ISSN: 0975-0983(Online); 0376-4699(Print)
Appears in Collections:IJC-B Vol.60B(08) [August 2021]

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