(S)-2-amino-3-(benzyloxy)-N-(4-(4-fluorophenoxy)phenyl)propanamide → (S)-2-(2-(1H-benzo[d][1,2,3]triazol-1-yl)acetamido)-3-(benzyloxy)-N-(4-(4-fluorophenoxy)phenyl)propanamide

関与物質

反応手順

Proceeding as in Example 1, but substituting 2-(1H-benzo[d][1,2,3]triazol-1-yl)acetic acid hydrochloride and (S)-2-amino-3-(benzyloxy)-N-(4-(4-fluorophenoxy)phenyl)propanamide, gave Compound 151, (S)-2-(2-(1H-benzo[d][1,2,3]triazol-1-yl)acetamido)-3-(benzyloxy)-N-(4-(4-fluorophenoxy)phenyl)propanamide (41 mg, 59%); Major isomer: 1H-NMR (400 MHz, DMSO-D6): σ 10.25 (br s, 1H), 9.04-9.02 (d, 1H), 8.05-8.03 (d, 1H), 7.78-7.76 (d, 1H), 7.64-7.60 (d, 2H), 7.53-7.49 (t, 1H), 7.41-7.38 (t, 1H), 7.33-7.28 (m, 5H), 7.23-7.19 (t, 2H), 7.05-6.98 (m, 4H), 5.59 (s, 1H), 4.77-4.72 (m, 1H), 4.56 (s, 1H), 3.73-3.72 (d, 2H). MS (EI) for C30H26FN5O4. found 540.0 (MH+).

情報源と証拠