Toluene-4-sulfonic acid 2-(2-biphenyl-4-yl-methyl-oxazol-4-yl)ethyl ester → 3-(4-[2-(2-Biphenyl-4-yl-5-methyl-oxazol-4-yl)-ethoxy]-2-{[(2,5-dichloro-thiophene-3-carbonyl)-amino]-methyl}-phenyl)-propionic acid tert-butyl ester

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A mixture of 3-(2-{[(2,5-dichloro-thiophene-3-carbonyl)-amino]-methyl}-4-hydroxy-phenyl)-propionic acid tert-butyl ester (280 mg, 0.651 mmol) and toluene-4-sulfonic acid 2-(2-biphenyl-4-yl-5-methyl-oxazol-4-yl)-ethyl ester (498 mg, 1.15 mmol), were reacted according to Standard procedure A to give, after radial chromatography (hexanes/EtOAc 98:2 to 90:10), the title compound as a white solid (367 mg, 82%). 1H NMR (400 MHz, CDCl3): 1.36 (s, 9H), 2.37 (s, 3H), 2.55 (t, 2H, J=7.3 Hz), 2.87 (t, 2H, J=7.3 Hz), 2.96 (t, 2H, J=6.6 Hz), 4.22 (t, 2H, J=6.8 Hz), 4.58 (d, 2H, J=5.4 Hz), 6.80 (dd, 1H, J=8.3 Hz, J=2.4 Hz), 6.88 (d, 1H, J=2.9 Hz), 6.97 (t, 1H, J=5.9 Hz), 7.10 (d, 1H, J=8.8 Hz), 7.13 (s, 1H), 7.36 (t, 1H, J=7.3 Hz), 7.45 (t, 2H, J=7.8 Hz), 7.63 (d, 2H, J=8.3 Hz), 7.65 (d, 2H, J=6.3 Hz), 8.02 (d, 2H, J=7.8 Hz). MS (ES) m/e 691.2 [M+1].

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