2-Methyl-3-butyn-2-ol → (+/-)-3-((1,3-dimethyl-1H-pyrazol-4-yl) (hydroxy)methyl)-9-fluoro-10-(3-hydroxy-3-methylbut-1-yn-1-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepine-2-carboxamide

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Reaction Steps

3-((1,3-dimethyl-1H-pyrazol-4-yl)(hydroxy)methyl)-9-fluoro-10-(3-hydroxy-3-methylbut-1-yn-1-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepine-2-carboxamide was prepared similarly according to General Procedure G with slight modifications. 10-bromo-3-((1,3-dimethyl-1H-pyrazol-4-yl)(hydroxy)methyl)-9-fluoro-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepine-2-carboxamide was reacted with 3-methyl-1-butyne-3-ol to afford 11.3 mg of the titled compound (19% yield). M+1=436.1. 1H NMR (400 MHz, DMSO) δ 8.58 (d, J=8.5 Hz, 1H), 7.87 (br s, 1H), 7.40 (br s, 1H), 7.25 (s, 1H), 6.99 (d, J=10.5 Hz, 1H), 6.72 (d, J=6.3 Hz, 1H), 6.52 (d, J=6.2 Hz, 1H), 5.54 (s, 1H), 4.58-4.25 (m, 4H), 3.65 (s, 3H), 2.06 (s, 3H), 1.49 (s, 6H).

Provenance & Evidence