Methyl 2-aminopyridine-3-carboxylate → 6-{3-[7-Fluoro-2-(4-fluoro-benzyl)-3-oxo-2,3-dihydro-1H-isoindol-1-yl]-propionylamino}-nicotinic acid methyl ester

Participants

Reaction Steps

The product from Example 11, Part D (331 mg, 1 mmol) and 2-aminonicotinic acid methyl ester (316 mg, 2.1 mmol) were converted to the title compound in a manner analogous to the method described in Example 7, Part E without crystallization (269 mg, 58%). 1H NMR (300 MHz, CDCl3) δ 8.83 (d, J=2 Hz, 1H), 8.27 (dd, J=8 Hz, 2 Hz, 1H), 8.16 (d, J=9 Hz, 1H), 7.87 (br s, 1H), 7.69 (d, J=7 Hz, 1H), 7.46 (m, 1H), 7.31 (m, 2H), 7.20 (t, J=9 Hz, 1H), 7.02 (t, J=9 Hz, 2H), 5.25 (d, J=15 Hz, 1H), 4.70 (m, 1H), 4.25 (d, J=15 Hz, 1H), 3.92 (s, 3H), 2.52 (m, 2H), 1.98 (m, 2H). MS: m/z (MH+) 466.

Provenance & Evidence