Yield:478076-57-2 68%

Reaction Conditions:

with potassium carbonate in DMF (N,N-dimethyl-formamide) at 140; for 18 h;

Steps:

230A Example 230A; 2'-Fluoro-6'-benzylaminobutyrophenone

2',6'-Difluorobutyrophenone (10 g, 54 mmol) is dissolved in DMF (110 ml) under a nitrogen atmosphere, in the presence of benzylamine (5.9 ml; 54 mmol) and potassium carbonate (11 g; 81 mmol). The mixture is stirred for 18 hours at 140° C. The reaction mixture is then cooled, neutralized by addition of water and extracted three times with ethyl acetate. The organic phases are combined, dried over magnesium sulfate, filtered and concentrated to give the desired product (10.3 g; 68%). [0350] 1H NMR, DMSO-d6 (ppm): 8.90 (t, 1H); 7.4-7.1 (m, 6H); 6.52 (d, 1H); 6.40 (dd, 1H); 4.45 (d, 2H); 2.85 (t, 2H); 1.62 (sext., 2H); 0.91 (t, 3H).

References:

US2004/204417,2004,A1 Location in patent:Page 50