5-((Tert-butoxycarbonyl)amino)-2-(2,6-difluorophenyl)thiazole-4-carboxylic acid → HCID 74983240, compound

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Reaction Steps

Following the procedure for Example 101 starting from tert-butyl 4-methyl-1-(1-methyl-4-nitro-1H-pyrazol-5-yl)azepan-4-ylcarbamate and 5-(tert-butoxycarbonylamino)-2-(2,6-difluorophenyl)-thiazole-4-carboxylic acid gave 411 as a pale brown solid (68 mg, 55% over three steps). 1H NMR (400 MHz, CDCl3) δ 8.98 (s, 1H), 7.91 (s, 1H), 7.38-7.25 (m, 1H), 7.02 (t, J=8.7 Hz, 2H), 6.20 (s, 2H), 3.73 (s, 3H), 3.34-3.26 (m, 1H), 3.33-3.08 (m, 2H), 3.17-3.09 (m, 1H), 1.95-1.78 (m, 2H), 1.77-1.66 (m, 4H), 1.19 (s, 3H). Exchangeable NH2 not observed. LCMS (ES+) m/z 462 (M+1)

Provenance & Evidence