A concise and efficient synthesis of vildagliptin

Autor:	Giovanni B. Giovenzana, Michele Castaldi, Ivan Guglielmo Menegotto, Graziano Castaldi, Marco Baratella
Rok vydání:	2017
Předmět:	010405 organic chemistry Stereochemistry Organic Chemistry 010402 general chemistry 01 natural sciences Biochemistry 0104 chemical sciences chemistry.chemical_compound chemistry Reaction sequence Yield (chemistry) Drug Discovery medicine Vildagliptin Glyoxylic acid medicine.drug
Zdroj:	Tetrahedron Letters. 58:3426-3428
ISSN:	0040-4039
DOI:	10.1016/j.tetlet.2017.07.062
Popis:	An original synthesis of vildagliptin (( S )-1-[2-(3-hydroxyadamantan-1-ylamino)acetyl]pyrrolidine-2-carbonitrile), a powerful DPP-4 inhibitor, was developed. Vildagliptin was assembled from 3-amino-1-adamantanol, glyoxylic acid and l -prolinamide in a 4-step reaction sequence with the isolation of only two intermediates. The procedure is competitive with existing protocols, leading to vildagliptin in 63% overall yield.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::00748db0ca4fc810d4e35053fc220755 https://doi.org/10.1016/j.tetlet.2017.07.062 Zobrazit plný text záznamu Full Text from ScienceDirect