| 摘要 |
<p>Producing 2,2-difluoroethylamine derivatives (III) comprises hydrogenating 2,2-difluoroethylamine derivatives (IV) to corresponding 2,2-difluoroethylamine derivatives (III). Producing 2,2-difluoroethylamine derivatives of formula (R 1>(A)(R 2>)-NHC-C(F)(F)) (III) comprises hydrogenating 2,2-difluoroethylamine derivatives of formula (R 1>(A)(R 2>)-N=C-C(F)(F)) (IV) to corresponding 2,2-difluoroethylamine derivatives of formula (R 1>(A)(R 2>)-NHC-C(F)(F)) (III). An independent claim is also included for producing 2,2-difluoroethylamine derivatives of formula (R 1>(A)(R 2>)-N=C-C(F)(F)) (IV) comprising performing condenstaion reaction of amine of formula (R 1>-C(A)(R 2>)-NH 2) (VI) with 2,2-difluoracetaldehyde or its derivative of formula (R 3>-O-CH(O-R 4>)-CH(F)(F)) (VIIa), (R 3>-O-CH(OH)-CH(F)(F)) (VIIb), (R 4>-O-CH(OH)-CH(F)(F)) (VIIc), difluoro derivative of formula (VIId), (CH(OH)(OH)-CH(F)(F)) (VIIe) or (R 3>-C(=O)-O-CH(O-C(=O)(R 4>))-CH(F)(F)) (VIIf). A : pyrid-2-yl or pyrid-4-yl or pyrid-3-yl, which is optionally substituted in 6-position by fluorine, chlorine, bromine, methyl, trifluoromethyl or trifluoromethoxy, pyridazine-3-yl, which is optionally substituted in 6-position by chlorine or methyl, pyrazine-3-yl, 2-chloro-pyrazine-5-yl or 1,3-thiazol-5-yl, which is optionally substituted in 2-position by chlorine or methyl, pyrimidinyl, pyrazolyl, thiophenyl, oxazolyl, isoxazolyl, 1,2,4-oxadiazolyl, isothiazolyl, 1,2,4-triazolyl or 1,2,5-thiadiazolyl, which is optionally substituted by fluorine, chlorine, bromine, cyano, nitro, 1-4C alkyl (which is optionally substututed by fluorine and/or chlorine), 1-3C-alkylthio (which is optionally substituted by fluorine and/or chlorine), or 1-3C alkylsulfonyl (which is optionally substituted by fluorine and/or chlorine) or pyridine compound of formula (V); X : halo, alkyl or haloalkyl; Y : halo, alkyl, haloalkyl, haloalkoxy, azido or cyano; R 1>, R 2>, R 3>, R 4> : H or 1-6C alkyl; and n : 0-2. [Image].</p> |
