发明名称 Process for preparing 2,2-difluoroethylamine derivatives by alkylating 2,2-difluoroethylamine
摘要 A method for preparing a 2,2-difluoroethylamine of the formula (III) in which 2,2-difluoroethylamine of the formula (I) is reacted with a halide of the formula (II) in the presence of a tertiary nitrogen base:; where, in the formulae (II) and (III), Hal and A are defined as stated in the description.
申请公布号 US9376389(B2) 申请公布日期 2016.06.28
申请号 US201314411173 申请日期 2013.06.24
申请人 Bayer Cropscience AG 发明人 Funke Christian;Lui Norbert;Warsitz Rafael;Schnatterer Albert
分类号 C07D213/61 主分类号 C07D213/61
代理机构 McBree Moore Woodward Vanik IP, LLC 代理人 McBree Moore Woodward Vanik IP, LLC
主权项 1. A method for preparing a 2,2-difluoroethylamine of formula (III) comprising reacting 2,2-difluoroethylamine of formula (I) with a halide of formula (II) wherein Hal is chlorine, bromine or iodine, in the presence of diisopropylethylamine, wherein, in the formulae (II) and (III) A is a pyrid-2-yl, pyrid-4-yl or pyrid-3-yl radical each of which may be substituted in the 6-position by fluorine, chlorine, bromine, methyl, trifluoromethyl or trifluoromethoxy or is pyridazin-3-yl, which may be substituted in the 6-position by chlorine or methyl, or is a pyrazin-3-yl, 2-chloropyrazin-5-yl or 1,3-thiazol-5-yl radical, which may respectively be substituted in the 2-position by chlorine or methyl, or is a pyrimidinyl, pyrazolyl, thiophenyl, oxazolyl, isoxazolyl, 1,2,4-oxadiazolyl, isothiazolyl, 1,2,4-triazolyl or 1,2,5-thiadiazolyl radical, which may be substituted by fluorine, chlorine, bromine, cyano, nitro, C1-C4-alkyl optionally substituted by fluorine and/or chlorine, C1-C3-alkylthio optionally substituted by fluorine and/or chlorine, or C1-C3-alkylsulphonyl optionally substituted by fluorine and/or chlorine, or is a pyrid-3-yl of the following formulawherein X is fluorine, chlorine, bromine, iodine, C1-C6-alkyl or C1-C6-haloalkyl and Y is fluorine, chlorine, bromine, iodine, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-haloalkoxy, azido or cyano.
地址 Monheim DE