2-(1H-1,2,4-triazol-1-yl)acetic acid hydrochloride → (S)-benzyl 4-(2-(1H-1,2,4-triazol-1-yl)acetamido)-5-(4-(4-fluorophenoxy)phenylamino)-5-oxopentylcarbamate

Participants

Reaction Steps

Proceeding as in Example 1, but substituting (S)-benzyl 4-amino-5-(4-(4-fluorophenoxy)phenylamino)-5-oxopentylcarbamate and 2-(1H-1,2,4-triazol-1-yl)acetic acid hydrochloride, gave Compound 165, (S)-benzyl 4-(2-(1H-1,2,4-triazol-1-yl)acetamido)-5-(4-(4-fluorophenoxy)phenylamino)-5-oxopentylcarbamate (90.1 mg, 20%). 1H-NMR (400 MHz, DMSO-D6): σ 10.19 (s, 1H), 8.69 (d, 1H), 8.48 (s, 1H), 7.96 (s, 1H), 7.60 (d, 2H), 7.39-7.29 (m, 5H), 7.21 (m, 2H), 7.04-6.96 (m, 4H), 5.00-4.97 (m, 4H), 4.46-4.39 (m, 1H), 3.04-2.99 (m, 2H), 1.75-1.39 (m, 4H). MS (EI) for C29H29FN6O5. found 560.9 (MH+).

Provenance & Evidence