3-Methoxytyramine → {3-[(3-{2-[2-(4-Hydroxy-3-methoxy-phenyl)-ethylamino]-pyrimidin-4-yl}-benzyl)-methanesulfonyl-amino]-propyl}-carbamic acid tert-butyl ester

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Reaction Steps

Intermediate 4 was coupled to 4-(2-Amino-ethyl)-2-methoxy-phenol following procedure F. LC-MS showed the product had the expected M+H+ of 586. 1H NMR (Varian 300 MHz, CDCl3, shifts relative to the solvent peak at 7.24 ppm) δ 8.28 (s, 1H) 8.05 (s, 1H) 7.96 (s, 1H) 7.50 (m, 2H) 7.0 (m, 1H) 6.83 (m, 1H) 6.77 (m, 2H) 5.64 (s, 1H) 4.84 (s, 1H) 4.44 (s, 3H) 4.09 (s, 2H) 3.86 (s, 2H) 3.77 (m, 1H) 3.25 (m, 3H) 3.07 (br s, 2H) 2.90 (m, 2H) 2.85 (S, 3H) 1.60 (m, 2H) 1.39 (s, 9H).

Provenance & Evidence