5-Bromo-2-fluoro-3-pyridinecarbonyl chloride synthesis

Yield:1256914-07-4 100%

Reaction Conditions:

with oxalyl dichloride;N,N-dimethyl-formamide in dichloromethane at 20; for 16 h;Inert atmosphere;

Steps:

2.1 Step 1) preparation of 5-bromo-2-fluoronicotinoyl chloride (Compound (Vc))

To a 1000 m L three neck glass flask with N₂protected was charged 5-bromo-2- fluoronicotinic acid (25 g, 110 mmol, 1 eq), DCM (330 g, 250 mL), DMF (66 g, 50 mL) and oxalyl chloride (23.6 g, 16.2 mL, 182 mmol, 1.65 eq). The mixture was stirred at 20^oC over 16 hours. The result mixture was concentrated under vacuum to afford crude product of formula (Vc) (26.3 g, 110 mmol, 100 % yield). The crude product was used in the next step directly.

References:

WO2022/78923,2022,A1 Location in patent:Page/Page column 15; 16