反应详情

To a solution of the 4-formylbenzoic acid in a suitable solvent such as dichloromethane, DMF or THF was added diisopropylethylamine (3 eq) and 3-[(dimethyliminium)-(dimethylamino)methyl]-1,2,3-benzotriazol-1-ium-1-olate hexafluorophosphate (HBTU) (1.1 eq). The reaction was allowed to stir for 30 min before ethyl or methyl-3-aminopropionate hydrochloride (1.1 eq) was added. The solution was stirred at room temperature for 4 hours. The solvents were evaporated under reduced pressure. The residue was taken up in ethyl acetate and 1N hydrochloric acid. The organic layer was separated and washed with water (2×), aqueous sodium hydrogen carbonate (3×), brine (2×), dried over magnesium sulphate and concentrated to give the desired product.

1. additionwas added
2. customThe solvents were evaporated under reduced pressure
3. customThe organic layer was separated
4. washwashed with water (2×), aqueous sodium hydrogen carbonate (3×), brine (2×)
5. dry with materialdried over magnesium sulphate
6. concentrationconcentrated