[2-(4-Bromo-phenyl)-6-trifluoromethyl-imidazo[1,2-a]pyridin-3-yl]-methanol synthesis

Yield:-

Reaction Conditions:

Stage #1:formaldehyd;2-(4-bromophenyl)-6-(trifluoromethyl)imidazo[1,2-a]pyridine hydrobromide with sodium acetate;acetic acid in water at 50; for 4 h;
Stage #2: with sodium hydroxide in water

Steps:

23
The intermediate (0.21 g, 0.50 mmol) was treated with 12.3 M formaldehyde in water (0.32 mL, 4.0 mmol) and sodium acetate (0.20 g, 2.5 mmol) in acetic acid (2 mL) at 50 °C for 4 h. The mixture was added to 1 M NaOH (100 mL) and was left with stirring overnight. The precipitate was collected by filtration, washed with water until the filtrate was neutral, and dried in vacuo to give the title compound as an off-white solid (163 mg). HRMS (ESI+) calcd for C₁₅Hi₀BrF₃N₂O 369.9929, found 369.9938.

References:

PROXIMAGEN LTD.;NILSSON, Marianne;HARALDSSON, Martin;HENRIKSSON, Sofia;EMOND, Rikard;SAVORY, Edward;SIMPSON, Iain WO2010/64020, 2010, A1 Location in patent:Page/Page column 41