2-Bromo-4-(trifluoromethyl)pyridine → N2-methyl-N-{(3aR,4S,6aS)-2-[4-(trifluoromethyl)pyrimidin-2-yl]octahydrocyclopenta[c]pyrrol-4-yl}-L-leucinamide

関与物質

反応手順

The title compound was prepared by substituting tert-butyl methyl((S)-4-methyl-1-((3aR,4S,6aS)-octahydrocyclopenta[c]pyrrol-4-ylamino)-1-oxopentan-2-yl)carbamate from Example 619 Step 1 for (2S,4S)-tert-butyl 4-fluoro-2-((3aR,4S,6aS)-octahydrocyclopenta[c]pyrrol-4-ylcarbamoyl)pyrrolidine-1-carboxylate and 2-bromo-4-(trifluoromethyl)pyrimidine for 2-bromo-4-(trifluoromethyl)pyridine in the procedure described in Example 637: 1H NMR (400 MHz, pyridine-d5) δ ppm 8.49 (d, J=4.8, 1H), 7.75-7.64 (m, 1H), 6.74 (d, J=4.8, 1H), 4.29 (dt, J=14.2, 7.2, 1H), 3.83 (d, J=4.5, 1H), 3.75 (dd, J=11.9, 8.2, 1H), 3.46 (dd, J=11.9, 4.8, 1H), 3.17-3.09 (m, 1H), 2.83-2.65 (m, 2H), 2.38 (s, 3H), 2.19-2.09 (m, 1H), 2.01-1.89 (m, 1H), 1.84 (dq, J=13.1, 6.6, 1H), 1.73-1.60 (m, 2H), 1.56-1.37 (m, 2H), 0.93 (d, J=6.6, 3H), 0.89 (d, J=6.6, 3H); MS (ESI+) m/z 400 (M+H)+.

情報源と証拠