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5H-Pyrano[4,3-b]pyridin-3-amine,7,8-dihydro-(9CI) synthesis

2synthesis methods
-

Yield:151225-39-7 95%

Reaction Conditions:

with palladium 10% on activated carbon;hydrogen in methanol at 20; under 750.075 Torr; for 16 h;Inert atmosphere;

Steps:

A18a Preparation of intermediate 101:

Intermediate 100 (1.30 g, 7.22 mmol) was dissolved in MeOH (77 mL) and the solution was degassed by N2 bubbling. Pd/C (10% wt, 767.89 mg, 0.72 mmol) was added and the mixture was hydrogenated under an atmosphere of H2 (1 bar) at rt for 16 h. The reaction mixture was filtered on a pad of celite and the solvent was removed under reduced presure to give 1.03 g of intermediate 101 (95% yield, brown solid) which was used in the next step without further purification.

References:

WO2018/2219,2018,A1 Location in patent:Page/Page column 284; 285