反应详情

To a solution of (3aR,7aS)-tert-butyl 5-(3-aminopyridin-4-yl)-2-oxohexahydrooxazolo[4,5-c]pyridine-3(2H)-carboxylate (1.0 equiv.) in DMF (0.3 M) was added 3-amino-6-(2,6-difluorophenyl)picolinic acid (1.2 equiv.), EDC (1.2 equiv.) and HOAt (1.2 equiv.). The solution was stirred for 15 h. To the mixture was added water and the precipitate was filtered. To the filtrate was added EtOAc, and the organic solution was extracted (3 times), dried with Na2SO4, and concentrated to give an orange syrup. The crude was triturated with EtOAc and hexanes mixture and the precipitate was filtered off to give pure product in 46% yield. LCMS (m/z): 567.0 (MH+), LC Rt=3.03 min.

1. filtrationthe precipitate was filtered
2. additionTo the filtrate was added EtOAc
3. extractionthe organic solution was extracted (3 times)
4. dry with materialdried with Na2SO4
5. concentrationconcentrated
6. customto give an orange syrup
7. customThe crude was triturated with EtOAc and hexanes mixture
8. filtrationthe precipitate was filtered off
9. customto give pure product in 46% yield