反应详情

Methyl 4-(2,4,5-trifluorophenyl)acetoacetate (21) was treated with anhydrous ammonium acetate in an alcoholic solvent, preferably methanol, and preferably at higher temperature, preferably at 60-65° C. The methyl(Z)-3-amino-4-(2,4,5-trifluorophenyl)but-2-enoate (28) formed was preferably isolated by complete removal of the solvent under reduced pressure, separation of excess of ammonium acetate by using a polar organic solvent such as ethyl acetate, distillation of the polar organic solvent and triturating the product with non-polar solvents like hexane.

1. custompreferably at 60-65° C