Diisopropylethylamine → 6-[2-(Methoxymethyl)pyrrolidin-1-yl]-5-methylnicotinonitrile

Participants

Reaction Conditions

Reaction Steps

2-(Methoxymethyl)pyrrolidine (406 mg; 3.53 mmol; 1.2 eq.) and DIEA (1.52 mL; 8.82 mmol; 3 eq.) were added to a solution of 5-cyano-2-fluoro-3-methylpyridine (400 mg; 2.94 mmol; 1 eq.) in 1-butanol (1 mL) and the reaction mixture was stirred at 90° C. for 16 hours. The reaction mixture was allowed to return to RT then diluted with EtOAc, washed with water, dried over MgSO4 and concentrated in vacuo to afford the title compound as a yellow oil (0.59 g, 87%). LC/MS (Method A): 200.1 (M+H)+. HPLC (Method A) Rt 2.42 min (Purity 99.1%).

Provenance & Evidence