ChemInform Abstract: Practical and Economical Approach to Synthesize Sitagliptin

ChemInform Abstract: Practical and Economical Approach to Synthesize Sitagliptin

The dipeptidyl peptidase 4 (DPP‐4) inhibitor sitagliptin phosphate monohydrate (V) is synthesized starting from compound (I) in an overall yield of 42% in four steps using the stereoselective reduction of compound (III) as the key step without the use of expensive and toxic catalysts or ligands.

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Veröffentlicht in:ChemInform 2014-03, Vol.45 (9), p.no-no
Hauptverfasser: Lin, Kuaile, Cai, Zhengyan, Zhou, Weicheng
Format: Artikel
Sprache:eng
Schlagworte:
diastereoselective syntheses
diastereoselective syntheses, enantioselective syntheses (incl. cis/trans‐isomerism)
enantioselective syntheses (incl. cis/trans-isomerism)
enzyme inhibiting activity
hydrogenation
pyrazine derivatives
reduction
reduction, hydrogenation
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Zusammenfassung:The dipeptidyl peptidase 4 (DPP‐4) inhibitor sitagliptin phosphate monohydrate (V) is synthesized starting from compound (I) in an overall yield of 42% in four steps using the stereoselective reduction of compound (III) as the key step without the use of expensive and toxic catalysts or ligands.
ISSN:0931-7597
1522-2667
DOI:10.1002/chin.201409186