(S)-1-((R)-2-(diethylamino)-2-phenylacetyl)-N-(4-(((4-fluorophenyl)(4-((S)-pyrrolidine-2-carboxamido)benzyl)amino)methyl)phenyl)pyrrolidine-2-carboxamide → N-(methoxycarbonyl)-O-methyl-L-threonyl-N-[4-({[4-({1-[(2R)-2-(diethylamino)-2-phenylacetyl]-L-prolyl}amino)benzyl](4-fluorophenyl)amino}methyl)phenyl]-L-prolinamide

Participants

Reaction Steps

The product from Example 81A (0.038 g, 0.054 mmol) and (2S,3R)-3-methoxy-2-(methoxycarbonylamino)butanoic acid (0.011 g, 0.059 mmol) were processed as in Example 81A to give 0.019 g (40%) of the title compound as an off-white solid. 1H NMR (500 MHz, DMSO-D6) δ ppm 0.89 (t, J=7.10 Hz, 3 H) 1.07 (t, J=7.17 Hz, 2 H) 1.13 (d, J=6.26 Hz, 3 H) 1.28 (t, J=7.25 Hz, 1 H) 1.76-1.92 (m, 4 H) 1.94-2.05 (m, 2 H) 2.07-2.23 (m, 2 H) 2.39-2.46 (m, 2 H) 2.57-2.63 (m, 2 H) 3.24 (s, 3 H) 3.34-3.42 (m, 1 H) 3.43-3.50 (m, 1 H) 3.53 (s, 3 H) 3.63-3.70 (m, 1 H) 3.75-3.87 (m, 2 H) 3.97-4.03 (m, 1 H) 4.26 (t, J=7.78 Hz, 1 H) 4.36-4.46 (m, 2 H) 4.56 (s, 4 H) 4.67 (s, 1 H) 6.64 (dd, J=9.31, 4.43 Hz, 2 H) 6.89-6.95 (m, 2 H) 7.16-7.22 (m, 4 H) 7.28 (t, J=7.17 Hz, 1 H) 7.33 (t, J=7.40 Hz, 2 H) 7.40 (d, J=7.17 Hz, 1 H) 7.49-7.57 (m, 4 H) 7.66-7.70 (m, 1 H) 9.96 (d, J=7.02 Hz, 2 H); MS ESI− m/z 876.5.

Provenance & Evidence