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    • 4. 发明授权
    • Process for the preparation of Sitagliptin
    • 西他列汀的制备方法
    • US08097724B2
    • 2012-01-17
    • US12727566
    • 2010-03-19
    • Pietro AllegriniEmanuele AttolinoGianmaria Dell'AnnaMario Michieletti
    • Pietro AllegriniEmanuele AttolinoGianmaria Dell'AnnaMario Michieletti
    • C07D491/00
    • C07D487/04
    • 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.
    • 制备式(I)化合物如2(R)-4-氧代-4- [3-(三氟甲基)-5,6-二氢[1,2,4]三唑并[4,3 -a] -7(8H) - 吡嗪基] -1-(2,4,5-三氟苯基)-2-丁胺或其盐以无水或水合的形式,作为对映异构体的混合物,或作为 包括将式(II)化合物或其盐转化成单一(R)或(S)对映异构体或其混合物,其中X为氢,羟基 C 1 -C 8烷基,C 1 -C 4烷氧基,芳基,氨基,N 3或卤素; (I)化合物,如果需要,将式(I)的单一对映体与外消旋混合物分离,和/或如果需要,将式(I)化合物转化为其盐 , 或相反亦然。