反应详情

温度

0 °C

To diisopropylamine (0.13 ml) in THF (8 ml) was dropwise added 1.62M n-butyllithium-hexane solution (1.2 ml) at -78° C., followed by stirring at 0° C. for 0.5 hour. The reaction mixture was cooled to -30° C., dropwise added with (S)-(-)-4methoxyphenyl methyl sulfoxide (157 mg) in THF (8 ml), and stirred at 0° C. for 0.5 hour. The reaction mixture was cooled to -78° C., added with N-(3-phenylpropionyl)-L-prolyl-L-proline benzyl ester (400 mg) in THF (8 ml) quickly, and stirred for 0.5 hour. The reaction mixture was treated as in Example 13-A) and the residue obtained was purified by medium pressure liquid chromatography (silica gel, eluate; chloroform:methanol=99:1) to give 195 mg of the title compound (See Table 5).

1. customat -78° C.
2. temperatureThe reaction mixture was cooled to -30° C.
3. stirringstirred at 0° C. for 0.5 hour
4. temperatureThe reaction mixture was cooled to -78° C.
5. stirringstirred for 0.5 hour
6. additionThe reaction mixture was treated as in Example 13-A) and the residue
7. customobtained
8. customwas purified by medium pressure liquid chromatography (silica gel, eluate; chloroform:methanol=99:1)