反应详情

温度

160 °C

To a solution of 10-(8-aza-bicyclo[3.2.1]oct-3-yl)-3-bromo-10H-phenothiazine, 4i (50 mg, 0.13 mmol) in DMF (750 μL) was added zinc cyanide (15 mg, 0.13 mmol) and tetrakistriphenylphosphine palladium (4 mg), the solution was purged with nitrogen, and the mixture was heated in the microwave for 5 min at 160° C. The mixture was allowed to cool to rt, and purified via reverse phase HPLC (eluent: CH3CN in water containing 0.1% TFA) to yield title compound 10-(8-aza-bicyclo[3.2.1]oct-3-yl)-10H-phenothiazine-3-carbonitrile, 1aa as a TFA salt and as a mixture of endo and exo isomers. MS m/z (MH+) 334.1.

1. customthe solution was purged with nitrogen
2. temperatureto cool to rt
3. custompurified via reverse phase HPLC (eluent: CH3CN in water containing 0.1% TFA)