反应详情

To a solution of 100 mg—(1-methyl-2-phenoxy-ethoxy)-naphthalene-2-carboxylic acid in 1.5 ml abs. DMF under inert atmosphere 45 mg 1-hydroxybenzotriazole, 83 mg 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride and 70 μl of N,N-diisopropylethylamine were added at 0° C. After 30 minutes at 0° C. 36 mg of 2-aminoisobutyric acid methyl ester hydrochloride, followed by 70 μl of N,N-diisopropylethylamine were added. After 16 h at room temperature the reaction mixture was concentrated, the residue was taken up in ethyl acetate and washed with 2 M HCl, aqueous sodium carbonate solution (10%) and brine. The organic layer was dried over magnesium sulphate, and concentrated to yield 114 mg of 2-methyl-2-{[1-(1-methyl-2-phenoxy-ethoxy)-naphthalene-2-carbonyl]-amino}-propionic acid methyl ester.

1. additionwere added
2. concentrationAfter 16 h at room temperature the reaction mixture was concentrated
3. washwashed with 2 M HCl, aqueous sodium carbonate solution (10%) and brine
4. dry with materialThe organic layer was dried over magnesium sulphate
5. concentrationconcentrated