A Novel Synthesis of (R)-3-(t-Butoxycarbonylamino)-4-(2,4,5- trifluorophenyl)butanoic Acid, a Key Intermediate, and the Formal Synthesis of Sitagliptin phosphate.
CHEMISTRY-AN ASIAN JOURNAL(2020)
摘要
An alternate formal synthesis of Sitagliptin phosphate is disclosed from 2,4,5-trifluorobenzadehyde in 8 linear steps with an overall yield of 31%. The chiral beta-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.
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关键词
Sitagliptin phosphate,Asymmetric Hydrogenation,Hoffmann rearrangement
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