Ethyl 2-aminopyridine-4-carboxylate → 2-{3-[7-Fluoro-2-(4-fluoro-benzyl)-3-oxo-2,3-dihydro-1H-isoindol-1-yl]-propionylamino}-isonicotinic acid ethyl ester

Participants

Reaction Steps

The product from Example 11, Part D (100 mg, 0.30 mmol) and 2-aminoisonicotinic acid ethyl ester (75 mg, 0.45 mmol) were converted to the title compound in a manner analogous to the method described in Example 7, Part E without crystallization (120 mg, 83%). 1H NMR (300 MHz, CDCl3) δ 8.61 (s, 1H), 8.31 (d, J=5 Hz, 1H), 7.81 (s, 1H), 7.70 (d, J=8 Hz, 1H), 7.58 (dd, J=5 Hz, 1 Hz, 1H), 7.47 (m, 1H), 7.32 (m, 2H), 7.20 (t, J=9 Hz, 1H), 7.02 (t, J=9 Hz, 2H), 5.27 (d, J=15 Hz, 1H), 4.71 (m, 1H), 4.41 (q, J=7 Hz, 2H), 4.24 (d, J=15 Hz, 1H), 2.55 (m, 2H), 1.97 (m, 2H), 1.41 (t, J=7 Hz, 3H). MS: m/z (MH+) 480.

Provenance & Evidence