3-Oxetanamine → 9-Fluoro-3-(hydroxymethyl)-10-(3-hydroxy-3-methyl-but-1-ynyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-2-carboxamide

Participants

Reaction Steps

2-Carbamoyl-9-fluoro-10-(3-hydroxy-3-methyl-but-1-ynyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-3-carboxylic acid (0.09 g) was reacted with 3-oxetanamine, 3-methyl similar to as described in Example 2 to afford 17.9 mg of 9-fluoro-3-(hydroxymethyl)-10-(3-hydroxy-3-methyl-but-1-ynyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-2-carboxamide following reverse phase hplc purification. MS (Q1) 443 (M)+. 1H NMR (400 MHz, DMSO) δ 11.84 (s, 1H), 8.62 (d, J=8.4 Hz, 1H), 8.44 (s, 1H), 7.93 (s, 1H), 7.02 (d, J=10.5 Hz, 1H), 5.49 (s, 1H), 5.07-4.92 (m, 2H), 4.69 (d, J=6.1 Hz, 2H), 4.66-4.49 (m, 2H), 4.42 (d, J=6.1 Hz, 2H), 1.63 (s, 3H), 1.49 (s, 6H).

Provenance & Evidence