反应详情

To a solution of 1 g of 4-{(S)-3-tert-Butoxycarbonyl-2-[(4-hydroxy-7-methyl-quinoline-2-carbonyl)-amino]-propionyl}-piperazine-1-carboxylic acid ethyl ester and 350 mg of (S)-2-Hydroxy-propionic acid benzyl ester in 20 ml of THF, 764 mg of Triphenyl-phosphane and 507 mg of Diethyl azodicarboxylate was added and stirred for 2 h. Then, the reaction mixture was diluted with water and extracted with ethyl acetate. The organic phase was dried over MgSO4 and the solvents were removed under reduced pressure. The crude product was purified by chromatography on silica gel eluting with a gradient of n-heptane/ethyl acetate. The fractions containing the product were combined and the solvent evaporated under reduced pressure. Yield: 1.0 g.

1. extractionextracted with ethyl acetate
2. dry with materialThe organic phase was dried over MgSO4
3. customthe solvents were removed under reduced pressure
4. customThe crude product was purified by chromatography on silica gel eluting with a gradient of n-heptane/ethyl acetate
5. additionThe fractions containing the product
6. customthe solvent evaporated under reduced pressure