反应详情

N-{[4-((2R,3R)-1-(4-Fluorophenyl)-3-{[2-(4-fluorophenyl)-2-oxoethyl]thio}-4-oxoazetidin-2-yl)phenoxy]acetyl}glycine (20 mg, 0.037 mmol) was dissolved in 3 ml DCM. N-Methylmorpholine (9 μl, 0.082 mmol) and TBTU (14 mg, 0.044 mmol) were added. After 5 minutes, tert-butyl 4-methylleucinate (9 mg, 0.045 mmol) was added and the mixture was stirred for 2 h. Additional tert-butyl 4-methylleucinate (ca 3 mg, 0.015 mmol) was added. After 15 min, water (2 ml) was added and the mixture was acidified to a pH of 2 using 2M KHSO4. The aqueous phase was extracted with 2 ml DCM and the combined organic phases were washed with 3 ml water, dried over Na2SO4 and filtered. Removal of the solvent under reduced pressure gave the title compound. M/z: 724.

1. waitAfter 15 min
2. extractionThe aqueous phase was extracted with 2 ml DCM
3. washthe combined organic phases were washed with 3 ml water
4. dry with materialdried over Na2SO4
5. filtrationfiltered
6. customRemoval of the solvent under reduced pressure