反应详情

温度

130 °C

To methyl 6-(4-fluorobenzyl)-4-hydroxy-3,5-dioxo-5,6,7,8-tetrahydro-2,6-naphthyridine-1-carboxylate (0.178 g, 0.514 mmol) in wet methanol was added N,N-dimethylamine in MeOH (4.0 eq.). The reaction mixture was put in a microwave reactor where it was heated at 130° C. for 1.5 hours, after which the reaction mixture was concentrated under vacuum. The residue was purified by reverse phase HPLC eluting with 5%-95% acetonitrile (0.1% TFA) in H2O (0.1% TFA) to afford the title compound as a solid. Alternatively, the starting material can be treated with LiOH in 1:1:1 THF/MeOH/H2O to give the product.

1. customThe reaction mixture was put in a microwave reactor
2. concentrationafter which the reaction mixture was concentrated under vacuum
3. customThe residue was purified by reverse phase HPLC
4. washeluting with 5%-95% acetonitrile (0.1% TFA) in H2O (0.1% TFA)