反应详情

8-Fluoro-3-methyl-1-oxo-2-pyridin-3-yl-1,2-dihydro-isoquinoline-4-carboxylic acid benzyl ester (0.150 g, 0.386 mmol) was dissolved in methanol (2 mL) and added to 10% Palladium on Charcoal (10 mg). The reaction mixture was stirred under an atmosphere of hydrogen for 60 minutes at room temperature. The reaction mixture was filtered and was rotovaped to give the title compound (0.105 g; yield 91.2%) as a yellow oil. Alternatively, the title acid can be obtained directly under the same conditions according to the above described Pd-catalysed carbonylation in the presence of water instead of benzyl alcohol. LC-MS (m/z) 299.3 (MH+); tR=0.43. 1H NMR (500 MHz, CDCl3): 2.15 (s, 3H), 7.16 (m, 1H), 7.59 (m, 1H), 7.61-7.7 (m, 2H), 7.73 (m, 1H), 8.6 (br. s, 1H), 8.78 (br., 1H).

1. filtrationThe reaction mixture was filtered