5-benzyl-N-(3-chloro-4-fluorophenyl)-3-(2,4-difluorobenzyl)-4-oxotetrahydropyrimidine-1(2H)-carboxamide (51)

NH Nicky Hwang
HB Haiqun Ban
JC Junjun Chen
JM Julia Ma
HL Hui Liu
PL Patrick Lam
JK John Kulp
SM Stephan Menne
JC Jinhong Chang
JG Ju-Tao Guo
YD Yanming Du
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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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