- PROCESS FOR THE PRODUCTION OF SITAGLIPTIN
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A novel process is described for the synthesis of Sitagliptin, IUPAC name 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine, of formula (I).
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- PROCESS FOR THE PRODUCTION OF SITAGLIPTIN
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A novel process is described for the synthesis of Sitagliptin, lUPAC name 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1 2,4-triazolo[4,3-a]pyrazine, of formula (I).
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Page/Page column 14-15
(2012/11/14)
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- PREPARATION METHOD OF INTERMEDIATE OF SITAGLIPTIN
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The present invention provides a method which enables the simple, economical and high-yield production which is a key intermediate of antidiabetic drug Januvia.
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Page/Page column 4-5
(2012/08/07)
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- Process for the production of sitagliptin
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The present invention is directed to a process for the preparation of Sitagliptin, having formula (I)
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Page/Page column 13
(2012/03/26)
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- PROCESS FOR THE PREPARATION OF A CHIRAL BETA AMINOACID DERIVATIVE AND INTERMEDIATES THEREOF
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It comprises a process for the preparation of sitagliptin, or its pharmaceutically acceptable salts, or its solvates, including hydrates, comprising: a) coupling an halo-2,4,5-trifluorobenzene with a compound of formula (IV) to give N-protected sitagliptin; the coupling being carried out via the formation of an organocupric compound of the halo-2,4,5-trifluorobenzene or, alternatively, via the formation of a organozinc compound of a compound of formula (IV); where R1 is hydrogen or an amino protective group; R2 is an amino protective group; or alternatively R1 and R2 taken together form a phtalimido group; X is Br or I; and Y is Br, I or R3SO3- wherein R3 is (C1-C4)- alkyl, phenyl, or phenyl mono- or disubstituted by a (C1-C4)-alkyl radical; b) submitting the N-protected sitagliptin to a deprotection reaction; and c) optionally its conversion into a pharmaceutically acceptable salt. It also comprises new intermediate compounds useful in such preparation process.
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Page/Page column 21-22
(2010/09/17)
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