5-Amino-4,6-dichloropyrimidine → (R)-4-chloro-6-((1-methylpiperidin-3-yl)oxy)pyrimidin-5-amine

Participants

Reaction Conditions

Reaction Steps

Sodium t-butoxide (586.0 mg, 6.098 mmol) was added to a solution of 4,6-dichloropyrimidin-5-amine (500 mg, 3.049 mmol) and (3R)-1-methylpiperidin-3-ol (351.2 mg, 3.049 mmol) in THF (25.00 mL) at RT. The reaction mixture was heated at 70° C. overnight. The reaction mixture was quenched with 1 mL water and concentrated in vacuo. The residue was extracted with DCM and the combined organic extract were dried and concentrated in vacuo to afford (R)-4-chloro-6-((1-methylpiperidin-3-yl)oxy)pyrimidin-5-amine which was used in next step without further purification.

Provenance & Evidence