反应详情

To the solution of 3.12 g of methyl (2S)-2-(1,3-benzoxazol-2-ylamino)-3-(4-hydroxyphenyl)propionate in 50 ml of dimethylformamide 60% suspension of NaH in mineral oil (0.4 g) was added portionwise with stirring at room temperature under argon atmosphere. When the evolution of the gas ceased, the solution of 2-[4-methyl-2-(3,4,5-trimethoxyphenyl)-1,3-oxazol-5-yl]ethyl 4-toluenesulfonate (4.47 g, 10 mmol) in dimethylformamide was added dropwise. The mixture was heated at 80° C. with stirring. After cooling, the mixture was poured into 1 l of water and extracted several times with ethyl acetate. The combined extracts were washed with brine, dried over magnesium sulfate and the solvent was evaporated, to obtain crude methyl (2S)-2-(1,3-benzoxazol-2-ylamino)-3-[4-(2-[5-methyl-2-(3,4,5-trimethoxy-phenyl)-1,3-oxazol-4-yl]ethoxy)phenyl]propionate.

1. additionwas added portionwise
2. temperatureThe mixture was heated at 80° C.
3. stirringwith stirring
4. temperatureAfter cooling
5. extractionextracted several times with ethyl acetate
6. washThe combined extracts were washed with brine
7. dry with materialdried over magnesium sulfate
8. customthe solvent was evaporated