(3-ChloroiMidazo[1,2-a]pyridin-6-yl)Methanol synthesis

Yield:167884-21-1 68%

Reaction Conditions:

with N-chloro-succinimide in acetonitrile; for 4 h;

Steps:

18.a

To a suspension of imidazo[l,2-α]pyridin-6-ylmethanol (410 mg, 2.77 mmol, Maybridge) in acetonitrile (14 mL) was added NCS (388 mg, 2.91 mmol) in one portion. After 4 h, the reaction mixture was concentrated under reduced pressure and the residue was triturated with boiling 95:5 v/v EtOAc/MeOH and hot filtered. The filtrate was purified directly by silica gel chromatography (95:5 EtOAc/MeOH) to give 343 mg (68%) of (3-chloroimidazo[l,2-α]pyridin-6-yl)methanol as a pale yellow solid. MS(ES)+ m/e 182.7 [M+H]⁺.

References:

WO2008/14219,2008,A2 Location in patent:Page/Page column 56