反应详情

A solution of Part D product (40 mg, 0.127 mmol), EDC (48.6 mg, 0.254 mmol) and 1-(4-amino-2-methoxyphenoxy)-2-methylpropan-2-ol (26.8 mg, 0.127 mmol) in DMF (1.0 mL) was stirred at RT overnight. After K2CO3(35.0 mg, 0.254 mmol) was added, the reaction was stirred overnight. Then the mixture was diluted with EtOAc (˜25 mL), washed with water and brine, dried over anhydrous Na2SO4, and concentrated. The resulting brown solution was purified by prep. HPLC to give 10 mg of the title compound as a white solid after lyophilization: 1H NMR (400 MHz, CDCl3) δ7.72 (d, J=8.3 Hz, 2H), 7.60 (s, 1H), 7.42 (d, J=8.3 Hz, 2H), 6.94 (br. s., 2H), 6.80 (s, 1H), 4.66 (s, 2H), 3.91 (s, 3H), 3.83 (s, 2H), 1.34 (s, 6H); HPLC retention time: 2.918 min; LCMS (ES): m/z 428 [M+H]+.

1. washwashed with water and brine
2. dry with materialdried over anhydrous Na2SO4
3. concentrationconcentrated
4. customThe resulting brown solution was purified by prep