Invention Grant
- Patent Title: Process for the preparation of Sitagliptin
- Patent Title (中): 西他列汀的制备方法
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Application No.: US12727566Application Date: 2010-03-19
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Publication No.: US08097724B2Publication Date: 2012-01-17
- Inventor: Pietro Allegrini , Emanuele Attolino , Gianmaria Dell'Anna , Mario Michieletti
- Applicant: Pietro Allegrini , Emanuele Attolino , Gianmaria Dell'Anna , Mario Michieletti
- Applicant Address: IT Baranzate (MI)
- Assignee: Dipharma Francis S.r.l.
- Current Assignee: Dipharma Francis S.r.l.
- Current Assignee Address: IT Baranzate (MI)
- Agency: Rothwell, Figg, Ernst & Manbeck, P.C.
- Priority: ITMI2009A1149 20090630
- Main IPC: C07D491/00
- IPC: C07D491/00

Abstract:
A process for the preparation of a compound of formula (I) such as 2(R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]-7(8H)-pyrazinyl]-1-(2,4,5-trifluorophenyl)-2-butanamine, or a salt thereof, in the anhydrous or hydrated form, either as a mixture of enantiomers, or as a single (R) or (S) enantiomer, comprising the conversion of a compound of formula (II), or a salt thereof, either as a single (R) or (S) enantiomer or as a mixture thereof wherein X is hydrogen, hydroxy, C1-C8 alkyl, C1-C4 alkoxy, aryl, amino, N3 or halogen; into a compound of formula (I), and if desired, the separation of a single enantiomer of formula (I) from the racemic mixture, and/or, if desired, the conversion of a compound of formula (I) into a salt thereof, or vice versa.
Public/Granted literature
- US20100331541A1 PROCESS FOR THE PREPARATION OF SITAGLIPTIN Public/Granted day:2010-12-30
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