Aminopyrazine → 3-[7-Fluoro-2-(4-fluoro-benzyl)-3-oxo-2,3-dihydro-1H-isoindol-1-yl]-N-pyrazin-2-yl-propionamide

Participants

Reaction Steps

The product from Example 11, Part D (100 mg, 0.3 mmol) and pyrazin-2-ylamine (43 mg, 0.45 mmol) were converted to the title compound in a manner analogous to the method described in Example 7, Part E, using CH2Cl2 in place of THF in the reaction and EtOAc in the workup, and without crystallization (8 mg, 7%). 1H NMR (300 MHz, CDCl3) δ 9.42 (s, 1H), 8.31 (d, J=3 Hz, 1H), 8.15 (m, 1H), 7.83 (s, 1H), 7.68 (d, J=8 Hz, 1H), 7.46 (m, 1H), 7.32 (m, 2H), 7.20 (t, J=9, 1H), 7.02 (t, J=7 Hz, 2H), 5.25 (d, J=15 Hz, 1H), 4.71 (m, 1H), 4.25 (d, J=15 Hz, 1H), 2.61 (m, 1H), 2.52 (m, 1H), 2.00 (m, 2H). MS: m/z (MH+) 409.

Provenance & Evidence