5-CHLORO-3-FLUORO-2-METHOXY-PYRIDINE synthesis

Yield:886374-01-2 69.89%

Reaction Conditions:

with sodium methylate in methanol at 65; for 2 h;

Steps:

1.1 Step 1:

To a solution of compound 1 (1 g, 6.687mmol, 1 eq) in Dry Methanol (5ml_), a solution of 30% NaOMe (1 .8ml_, 10.03mmol, 1.5eq) was added dropwise and the reaction mixture was heated to 65°C for 2h (Reaction was monitored by 1 HNMR and LCMS). Then, the reaction mixture was cooled to RT and concentrated under reduced pressure to give a residue. Residue was dissolved in EtOAc and washed with water. The separated organic layer was dried over Na2S0₄ and concentrated under reduced pressure to give compound 2 (750mg, 69.89%) as colorless liquid; which was sufficiently pure to use for next step.

References:

WO2019/153080,2019,A1 Location in patent:Paragraph 00376