摘要 |
PURPOSE:To produce an acetamide derivative in extremely high yield by reacting an amine compound with an acetic acid halide in a water-organic solvent system in the presence of a phase-transfer catalyst. CONSTITUTION:The acetamide derivative of formula I is produced by reacting an amine compound of the formula HNR1R2 (R1 and R2 are H or 1-5C alkyl) and/or its inorganic acid salt with an acetic acid halide of the formula XCH2 COX' (X is H or halogen; X' is halogen) in the presence of an acid acceptor. The reaction is carried out in a water-organic solvent system in the presence of a phase transfer catalyst, preferably a substituted ammonium halide of formula II (R3 to R6 are H, 1-4C alkyl or benzyl; Y is halogen), e.g. benzyltriethylammonium chloride. The amount of the catalyst is usually 0.01-1mol, especially 0.05-0.15mol based on 1mol of the acetic acid halide. |