Efficient synthesis of Vildagliptin intermediates
By: Li, Yufei.
Contributor(s): Jiang, Lan.
Publisher: New Delhi CSIR 2021Edition: Vol.60(B), Aug.Description: 1128-1131p.Subject(s): GENERAL CHEMISTRYOnline resources: Click here In: Indian journal of chemistry (Section B)Summary: 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%.Item type | Current location | Call number | Status | Date due | Barcode | Item holds |
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Articles Abstract Database | School of Pharmacy Archieval Section | Not for loan | 2022-0284 |
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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