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

Beteiligte Stoffe

Reaktionsschritte

Proceeding as in Example 1, but substituting 2-(1H-1,2,4-triazol-1-yl)acetic acid hydrochloride and (2S,4R)-4-(2-chlorobenzyl)-N-(4-(4-fluorophenoxy)phenyl)pyrrolidine-2-carboxamide, gave Compound 57, (2S,4R)-1-(2-(1H-1,2,4-triazol-1-yl)acetyl)-4-(2-chlorobenzyl)-N-(4-(4-fluorophenoxy)phenyl)pyrrolidine-2-carboxamide (71 mg, 55%). Major isomer: 1H-NMR (400 MHz, DMSO-D6): σ 10.03 (s, 1H), 8.44 (s, 1H), 7.96 (s, 1H), 7.59-7.52 (m, 2H), 7.49-7.15 (m, 6H), 7.05-6.90 (m, 4H), 5.25 (q, 2H), 4.60-4.49 (m, 1H), 3.92-3.79 (m, 1H), 2.97-2.73 (m, 3H), 2.30-1.88 (m, 2H). MS (EI) for C28H25FN5O3. found 533.9 (MH+).

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