5-Iodo-3-methylpyridin-2-amine → 2-Cyclopropyl-6-iodo-3,8-dimethylimidazo[1,2-a]pyridine

反応式

[I:1][C:2]1[CH:3]=[C:4]([CH3:9])[C:5]([NH2:8])=[N:6][CH:7]=1.Br[CH:11]([CH3:17])[C:12]([CH:14]1[CH2:16][CH2:15]1)=O.[Cl-].[Cl-].[Ca+2]>CN(C=O)C>[CH:14]1([C:12]2[N:8]=[C:5]3[C:4]([CH3:9])=[CH:3][C:2]([I:1])=[CH:7][N:6]3[C:11]=2[CH3:17])[CH2:16][CH2:15]1

参加物

実験手順

A mixture of 5-iodo-3-methylpyridin-2-amine (100 mg), 2-bromo-1-cyclopropylpropan-1-one (113 mg) and DMF (1 ml) was stirred at 80° C. under a dry atmosphere (CaCl2 tube) overnight. The mixture was quenched with saturated NaHCO3 solution and extracted with EtOAc. The organic layer was separated, washed with water and brine, dried over MgSO4 and concentrated in vacuo. The residue was purified by NH silica gel column chromatography (hexane/EtOAc) to give the title compound (69.3 mg) as a pale yellow oil.