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    • 5. 发明申请
    • SYNTHESIS OF 4-AMINO-PYRIMIDINES
    • 4-氨基吡啶的合成
    • WO2008087021A1
    • 2008-07-24
    • PCT/EP2008/000320
    • 2008-01-17
    • DSM IP ASSETS B.V.BONRATH, WernerHAERTER, RalphKARGE, ReinhardLETINOIS, Ulla
    • BONRATH, WernerHAERTER, RalphKARGE, ReinhardLETINOIS, Ulla
    • C07D239/42
    • C07D239/42
    • Process for the manufacture of a compound of the structure (I) with R 1 = hydrogen, alkyl (C1 - C10, linear, cyclic or branched, aliphatic or aromatic), NR'R" (wherein R' and R" are independently selected from H, alkyl [C1 - C10, linear, cyclic or branched, aliphatic or aromatic] and R 2 = CH 2 R 3 wherein R 3 is selected from NHR1"' (with R"' = C(O)H, C(O)CH 3 , C(O)alkyl, CH 2 C 6 H 2 (OMe) 3 or other saponifiable residues), alkyl (C1 - C10, linear, cyclic or branched) aromatic residues, heteroaryl residues, substituted aryl residues, e. g. 3,4,5-trimethoxy-phenyl) wherein 1 equivalent of an α-formyl-propionitrile salt is reacted with 0.75 to 2 equivalents of an acetamidine salt in the presence of a Lewis acid.
    • 制备具有R 1 =氢的结构(I)的化合物的方法,(C1-C10,直链,环状或支链,脂族或芳族)烷基,NR'R“(其中R '和R“独立地选自H,烷基[C1-C10,直链,环状或支链,脂族或芳族]和R 2 = CH 2 3其中R 3选自NHR 1“(R”'= C(O)H,C(O)CH 3 N,C(O )烷基,CH 2 2 C 6 H 2(OMe)3或其它可皂化残基),烷基(C 1 -C 10,直链,环状或支链)芳族残基,杂芳基残基,取代的芳基残基,例如3,4,5-三甲氧基 - 苯基),其中1当量的α-甲酰基 - 丙腈盐与0.75-2当量的 乙脒盐在路易斯酸存在下反应。