2-Fluoro-5-methylbenzeneboronic acid → HCID 73603035, compound

Participants

Reaction Steps

Following the procedure for Example 108, (R)-tert-butyl 2-bromo-4-(1-(2,2-difluoroethyl)-5-(4-(2,2,2-trifluoro-N-methylacetamido)azepan-1-yl)-1H-pyrazol-4-ylcarbamoyl)thiazol-5-ylcarbamate (80 mg, 0.12 mmol) and 2-fluoro-5-methylbenzeneboronic acid (30 mg, 0.20 mmol) were reacted to give 119 as the mono formate salt as a pale pink solid (11 mg, 19% over two steps). 1H NMR (400 MHz, d4-MeOD) δ 8.56 (s, 1H), 8.08 (dd, J=7.3, 2.2 Hz, 1H), 7.60 (s, 1H), 7.26-7.20 (m, 1H), 7.12 (dd, J=11.4, 8.4 Hz, 1H), 6.41-6.08 (m, 1H), 4.54-4.43 (m, 2H), 3.40-3.33 (m, 3H), 3.32-3.24 (m, 2H), 2.64 (s, 3H), 2.41 (s, 3H), 2.33-1.94 (m, 3H), 1.91-1.76 (m, 3H). LCMS (ES+) m/z 508 (M+1).

Provenance & Evidence