反应详情

(2R,6S)-1,2,6-Trimethylpiperazine (105 mg, 0.52 mmol), cesium carbonate (680 mg, 2.09 mmol), BINAP (2.44 mg, 3.91 μmol) and Pd2(dba)3 (1.20 mg, 1.30 μmol) were added to 5-bromo-2-[(phenylmethyl)oxy]-N-3-pyridinylbenzamide (may be prepared as described in example 2; 200 mg, 0.52 mmol) in anhydrous toluene (5 ml), and the mixture was heated to reflux overnight. The reaction mixture was evaporated under reduced pressure. Water (50 ml) was added to the residue and the mixture was extracted with ethyl acetate (3×50 ml). The organics were combined and evaporated, and the residue purified by MDAP twice to yield the title compound. 180 mg.

1. temperaturethe mixture was heated
2. temperatureto reflux overnight
3. customThe reaction mixture was evaporated under reduced pressure
4. additionWater (50 ml) was added to the residue
5. extractionthe mixture was extracted with ethyl acetate (3×50 ml)
6. customevaporated
7. customthe residue purified by MDAP twice