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    • 10. 发明授权
    • Method of producing nitroguanidine- and nitroenamine derivatives
    • 制备硝基胍和硝基胺衍生物的方法
    • US06747146B2
    • 2004-06-08
    • US10325559
    • 2002-12-20
    • Gottfried SeifertThomas RapoldVerena Gisin
    • Gottfried SeifertThomas RapoldVerena Gisin
    • C07D27304
    • C07D213/40C07C257/22C07C261/00C07C277/08C07D213/38C07D277/28C07D307/14C07D401/06C07D417/06C07C279/36
    • Method of producing compounds of formula wherein R1 is hydrogen or C1-C4-alkyl; R2 is hydrogen, C1-C8-alkyl, C3-C6-cycloalkyl, or a radical —N(R3)R4; or R2 and R6 together are —CH2—CH2—S—; R3 and R4 are hydrogen, C1-C4-alkyl, C3-C6-cycloalkyl or a radical —CH2B; R6 is hydrogen, C1-C8-alkyl, aryl or benzyl; or R3 and R6 together are —CH2—CH2—, —CH2—CH2—CH2—, —CH2—O—CH2—, —CH2—S—CH2— or —CH2—N(R5)—CH2—; X is CH—CN; CH—NO2 or N—NO2; A is an optionally substituted, aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical; and B is optionally substituted phenyl, 3-pyridyl or thiazolyl; characterised in that a compound of formula wherein R2, R6 and X have the same significance as given above in formula (I), is reacted in the presence of a phase transfer catalyst and a base with a compound of formula wherein A and R1 have the same significance as given above in formula (I) and Q is a leaving group.
    • 制备糠醛的化合物的方法是氢或C 1 -C 4烷基; R 2是氢,C 1 -C 8烷基,C 3 -C 6环烷基或-N(R 3)R 4基团; 或R 2和R 6一起是-CH 2 -CH 2 -S-; R 3和R 4是氢,C 1 -C 4 - 烷基,C 3 -C 6环烷基或基团-CH 2 B; R 6是氢,C 1 -C 8 - 烷基,芳基或苄基 ;或R 3和R 6一起是-CH 2 -CH 2 - , - CH 2 -CH 2 - , - CH 2 -O-CH 2 - , - CH 2 -S-CH 2 - 或-CH 2 -N(R 5)-CH 2 - ; X是 CH-CN; CH-NO 2或N-NO 2; A是任选取代的芳族或非芳族单环或双环杂环基; 和B是任选取代的苯基,3-吡啶基或噻唑基;其特征在于,式(I)化合物与式(I)中所给出的具有相同意义的化合物在相转移催化剂和碱的存在下反应 与式(I)中的上述式相同,Q为离去基团。