反应详情

To 6-(2,4-dichlorophenyl)-5-(4-chlorophenyl)-2-(isobutylamino)pyridine-3-carbonitrile [prepared by reacting the product of Example 1 step C with isobutyl amine] (0.26 g) in TH (2.5 mL) was added MeMgBr (0.47 mL, 1.4 M solution in toluene THF 3:1) followed by propionyl chloride. After 1 hour 45 minutes the reaction was quenched with 2 M aqueous HCl, diluted with EtOAc and washed with saturated aqueous NaHCO3 solution. The dried solution (Na2SO4) was concentrated and purified via flash chromatography on silica gel eluted with 20% EtOAc in hexane affording the title compound. HPLC/MS: 486.2(M+1), 488.2 (M+3); Rt=4.60 min.

1. customAfter 1 hour 45 minutes the reaction was quenched with 2 M aqueous HCl
2. additiondiluted with EtOAc
3. washwashed with saturated aqueous NaHCO3 solution
4. concentrationThe dried solution (Na2SO4) was concentrated
5. custompurified via flash chromatography on silica gel
6. washeluted with 20% EtOAc in hexane affording the title compound