6-(Trifluoromethyl)nicotinic acid → N-(3-{2-[2-(3-Chloro-4-hydroxy-phenyl)-ethylamino]pyrimidin-4-yl}-benzyl)-N-isopropyl-6-trifluoromethyl-nicotinamide

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Reaction Steps

2-Chloro-4-(2-{4-[3-(isopropylamino-methyl)-phenyl}-pyrimidin-2-ylamino]-ethyl)-phenol (compound 132) was coupled with 6-trifluoromethyl-nicotinic acid following procedure D2. LC-MS showed the product had the expected M+H+ of 570. 1H NMR (Varian 300 MHz, CDCl3, shifts relative to the solvent peak at 7.24 ppm) δ 9.5 (s, 1H)) 8.6 (d, 1H) 8.5 (s, 1H) 8.2 (d, 1H) 8.1 (s, 1H) 7.9 (m, 2H) 7.5 (m, 1H) 7.4 (m, 2H) 7.2 (s, 1H) 6.9 (d, 1H) 5.7 (s, br, 1H) 3.9 (s, 2H) 3.7 (m, 2H) 3.1 (m, 1H) 3.0 (m, 2H) 1.2 (d, 6H).

Provenance & Evidence