1-(3-METHYLPYRIDIN-2-YL)PIPERAZINE synthesis

Yield:111960-11-3 98%

Reaction Conditions:

with hydrogenchloride in 1,4-dioxane at 0 - 20; for 3 h;Inert atmosphere;

Steps:

36.2 Step-2

To the stirred solution of tert-butyl4-(3-methyl-2-pyridyl)piperazine-1-carboxylate (560 mg,1.80 mmol) in 1,4-dioxane (5 mL), cooled to 0 °C, 4 N HCl in dioxane (1.8 mL, 7.2 mmol)was added under argon atmosphere. The reaction mixture was slowly warmed toRT andstirred for 3 h (TLC indicated complete consumption of starting material). The volatiles wereremoved under reduced pressure and the residue was washed with Et20 (50 mL) to give 1-(3-methyl-2-pyridyl)piperazine hydrochloride (350 mg, 98%) which was used for the next stepwithout any purification.

References:

WO2018/125961,2018,A1 Location in patent:Page/Page column 90; 91