According to the procedure for preparation of compound 21, 2-benzyl-3-((tert-butoxycarbonyl)amino)propanoic acid (60 mg, 0.215 mmol) was treated with 2,4-difluorobenzylamine (31 mg, 0.215 mmol), EDC·HCl (41 mg, 0.215 mmol), HOBt·H2O (33 mg, 0.215 mmol), and excess triethylamine, and then continued the same procedure to afford 51. 1H NMR (300 MHz, CDCl3): δ (ppm) 7.41–7.36 (m, 1H), 7.36–7.23 (m, 4H), 7.23–7.17 (m, 2H), 7.15–7.07 (m, 1H), 7.04–6.96 (m, 1H), 6.88–6.74 (m, 2H), 5.03–4.95 (m, 1H), 4.76–4.70 (m, 1H), 4.70–4.55 (m, 2H), 3.64–3.55 (m, 1H), 3.45–3.36 (m, 1H), 3.00–2.85 (m, 1H), 2.74–2.62 (m, 1H); Calculated for C25H21ClF3N3O2, 487.1; observed (M + H)+ 488.6.
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