2-(2H-1,2,3-triazol-2-yl)acetic acid hydrochloride → (2S,4R)-1-(2-(2H-1,2,3-triazol-2-yl)acetyl)-N-(4-(4-fluorophenoxy)phenyl)-4-(3-methoxybenzyl)pyrrolidine-2-carboxamide

関与物質

反応手順

Proceeding as in Example 1, but substituting 2-(2H-1,2,3-triazol-2-yl)acetic acid hydrochloride and (2S,4R)—N-(4-(4-fluorophenoxy)phenyl)-4-(3-methoxybenzyl)pyrrolidine-2-carboxamide, gave Compound 69, (2S,4R)-1-(2-(2H-1,2,3-triazol-2-yl)acetyl)-N-(4-(4-fluorophenoxy)phenyl)-4-(3-methoxybenzyl)pyrrolidine-2-carboxamide (180 mg, 93%). 1H-NMR (400 MHz, CDCl3): σ 9.15 (s, 1H), 7.71 (s, 2H), 7.42 (d, 2H), 7.00 (t, 2H), 6.93-6.89 (m, 4H), 6.80-6.72 (m, 4H), 5.32-5.23 (m, 1H), 4.84 (d, 1H), 4.80 (d, 1H), 3.81 (s, 3H), 3.51 (dd, 1H), 3.17 (t, 1H), 2.99-2.88 (m, 2H), 2.69-2.59 (m, 2H), 1.73-1.65 (m, 1H). MS (EI) for C29H28FN5O4. found 530.2 (MH+).

情報源と証拠