4-(4-methylpiperazin-1-yl)pyridin-2-amine synthesis

Yield:959986-12-0 85%

Reaction Conditions:

in 1-methyl-pyrrolidin-2-one at 225; for 0.416667 h;Microwave irradiation;

Steps:

A mixture of 4-chloro-pyridin-2-ylamine (1.65 g, 12.9 mmcl) and 1-methyl-piperazine (4.2 ml, 37.9 mmcl) in NMP (15 ml) was heated under microwave irradiation at 225 00 for 25 mins. The solvent was evaporated, the residue was dissolved in water (40mL) and 4M NaOH (15 mL) was added. The precipitate was filtered, washed with diethyl ether and dried to afford 4-(4-methyl-piperazin-1-yl)-pyridin-2-ylamine as a white solid (2.09 g, 85%), (M+H)=1 93. 4-(4-Methyl-piperazin-1 -yl)-pyridin-2-ylamine was converted to the title compound using essentially similar procudure as in stepN2, (M+H)=289.

References:

WO2015/4481,2015,A1 Location in patent:Page/Page column 101