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US 11,174,266 B2Granted
Efficient process for the preparation of sitagliptin
AssigneeF.I.S. Fabbrica Italiana Sintetici S.p.A.
InventorsTerry Shi, Sam Lou, Ottorino De Lucchi, Pierluigi Padovan
Life of this patent
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Abstract
Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine.
Claims12
A process for the preparation of Sitagliptin of formula (I) or salt thereof:
- comprising:
- A) cyanation of 2,4,5-trifluorobenzoyl fluoride of formula (III):
- to give the compound of formula (IV):
- B) conversion of the compound of formula (IV) prepared in step A) to the compound of formula (V):
- C) reduction of the compound of formula (V) prepared in step B) to the compound of formula (II):
- and
- D) conversion of 2,4,5-trifluorophenylacetic acid of formula (II) obtained in step C) to Sitagliptin of formula (I) or salt thereof.
4 more elements
A process for the preparation of 2,4,5-trifluorophenylacetic acid of formula (II) or salt thereof:
- comprising:
- A) cyanation of 2,4,5-trifluorobenzoyl fluoride of formula (III):
- to give the compound of formula (IV):
- B) conversion of the compound of formula (IV) prepared in the step A) to the compound of formula (V):
- C) reduction of the compound of formula (V) prepared in the step B) to the compound of formula (II):
2 more elements
A process for the preparation of 2,4,5-trifluorophenylacetic acid of formula (II) or salt thereof:
- by direct conversion of the compound of (V):
- to the compound of formula (II),
- wherein said direct conversion is carried out by reduction reaction.
Dependencies are inferred from the claim text.