Kurella Sreenivasulu, Pramod S. Chaudhari, S. Achanta
Mar 3, 2020
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0
Influential Citations
2
Citations
Journal
Chemistry, an Asian journal
Abstract
An alternate formal synthesis of Sitagliptin phosphate is disclosed from 2,4,5-trifluorobenzadehyde in 8 linear steps with an overall yield of 31.16%. The chiral β-amino acid moiety present in sitaglitpin is installed via an asymmetric hydrogenation followed by a stereoselective Hofmann rearrangement as the key steps. The key chiral intermediate Boc-amino acid 1 prepared by this novel route was further converted to Sitagliptin phosphate following the known literature protocol.