反应详情

28 mg (0.065 mmol) of 1 (4S)-4-(2-aminoethyl)-6-(3-methylphenyl)-7-[3-(trifluoromethoxy)phenyl]-3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one hydrochloride were dissolved in 2 ml of DCM. To the obtained solution, 20 μl (0.20 mmol) of t-butyl isocyanate, 60 μl (0.33 mmol) of DIPEA, were added. The mixture was stirred at rt for 18 hours, the solution was portioned between ethyl acetate and saturated aqueous solution of NaHCO3, the organic layer was washed with brine, dried over Na2SO4 and evaporated under vacuum. The crude was purified by HPLC preparative method 1, to provide 1-tert-butyl-3-(2-{(4S)-6-(3-methylphenyl)-1-oxo-7-[3-(trifluoromethoxy)phenyl]-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazin-4-yl}ethyl)urea 12 mg (35%) as a white solid.

1. washthe organic layer was washed with brine
2. dry with materialdried over Na2SO4
3. customevaporated under vacuum
4. customThe crude was purified by HPLC preparative method 1