6-{3-[7-Fluoro-2-(4-fluorobenzyl)-3-oxo-2,3-dihydro-1H-isoindol-1-yl]-propionylamino}-nicotinic acid → 3-(6-{3-[7-Fluoro-2-(4-fluoro-benzyl)-3-oxo-2,3-dihydro-1H-isoindol-1-yl]-propionylamino}-pyridin-3-yl)-acrylic acid ethyl ester

Participants

Reaction Steps

The product of Example 11, Part D (137 mg, 0.41 mmol) and 3-(6-amino-pyridin-3-yl)-acrylic acid ethyl ester (80 mg, 0.41 mmol) were converted to the title compound in a manner analogous to the method described in Example 27 (90.8 mg, 43%). 1H NMR (400 MHz, CDCl3) δ 8.3 (s, 1H), 8.18 (d, J=8.7 Hz, 1H), 8.03 (s, 1H); 7.89-7.86 (d, J=8.6 Hz, 1H); 7.71 (d, J=7 Hz, 1H); 7.62 (d, J=16 Hz, 1H), 7.49-7.44 (m, 1H); 7.34 (m, 2H); 7.23 (t, J=8.75 Hz, 1H); 7.04 (t, J=8.8 Hz, 2H); 6.44 (d, J=16 Hz, 1H); 5.28 (d, J=15 Hz, 1H), 4.70 (m, 1H), 4.29-4.23 (m, 3H); 2.57-2.50 (m, 2H); 2.04-1.93 (m, 2H); 1.36 (t, J=7.4 Hz, 3H) MS: m/z (MH+) 506.

Provenance & Evidence