反应详情

A solution of Compound 85 (245 mg, 0.413 mmol) in DMF (5 mL) was treated with NH4Cl (180 mg, 3.3 mmol), DIEA (760 μl, 4.1 mmol) and HATU (170 mg, 0.4 mmol). After stirring overnight, the reaction mixture was diluted with EA (50 mL), washed with aq. 0.5 M HCl (100 mL) and brine (20 mL), then dried over MgSO4 and concentrated. The residue was re-slurried from ACN (4 mL) to afford 204 mg (77%) of (S)—N-(1-amino-3-(4-(5-(4-(heptyloxy)phenyl)pyrimidin-2-yl)phenyl)-1-oxopropan-2-yl)-4-(tert-butyl)benzamide as a fine white solid. LCMS-ESI (m/z) calculated for C37H44N4O3: 592.3. found 593.0 [M+H]+, tR=3.43 min (Method 6).

1. washwashed with aq. 0.5 M HCl (100 mL) and brine (20 mL)
2. dry with materialdried over MgSO4
3. concentrationconcentrated