1-(2-(Dimethylamino)ethyl)piperazine → 5-[6-({4-[2-(dimethylamino)ethyl]piperazin-1-yl}methyl)-1H-imidazo[4,5-c]pyridin-1-yl]-3-[(1R)-1-(2-fluorophenyl)ethoxy]thiophene-2-carboxamide

Participants

Reaction Conditions

Reaction Steps

136 mg of crude (1-{5-carbamoyl-4-[(1R)-1-(2-fluorophenyl)ethoxy]-2-thienyl}-1H-imidazo[4,5-c]pyridin-6-yl)methyl methanesulfonate (example 101, step 1) are dissolved in 5 ml dichloromethane. Under N2 atmosphere N,N-dimethyl-2-piperazin-1-ylethanamine (218 mg) is added. The reaction mixture is stirred at 40° C. for 2 hours and 2 hours at room temperature. It is then concentrated to dryness under vacuum. The residue is purified by preparative HPLC (ammonium formate buffer/acetonitrile, elution gradient 97/3 to 0/100 (v/v)) to obtain the title product.

Provenance & Evidence