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US08198443B2 Synthesis of 4-amino-pyrimidines scaffolds 有权
合成4-氨基 - 嘧啶支架

Synthesis of 4-amino-pyrimidines scaffolds
摘要:
Process for the manufacture of a compound of the structure (I) with R1=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 R2=CH2R3 wherein R3 is selected from NHR1′″ (with R′″=C(O)H, C(O)CH3, C(O)alkyl, CH2C6H2(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.
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