Piperidin-4-ol → (4-hydroxypiperidin-1-yl)(2-(1-isopropyl-1H-1,2,4-triazol-5-yl)-4,5-dihydrobenzo[b]pyrazolo[1,5-d][1,4]oxazepin-9-yl)methanone

Participants

Reaction Steps

Following the procedure for 116, 2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-1,10b-diaza-benzo[e]azulene-9-carboxylic acid was reacted with 4-hydroxy piperidine to give 118 as a white solid. 1H NMR (CDCl3, 400 MHz): δ 8.02 (d, J=2.1 Hz, 1 H); 7.94 (s, 1 H); 7.35 (dd, J=8.3, 2.1 Hz, 1 H); 7.23 (d, J=8.3 Hz, 1 H); 6.88 (s, 1 H); 5.76-5.62 (m, 1 H); 4.58 (t, J=5.8 Hz, 2 H); 4.19 (br s, 1 H); 4.07-3.98 (m, 1 H); 3.82 (br s, 1 H); 3.37 (br s, 2 H); 3.20 (t, J=5.8 Hz, 2 H); 1.95 (br s, 2 H); 1.70 (d, J=3.9 Hz, 1 H); 1.67-1.54 (d, J=6.6 Hz, 8 H). LCMS: RT=8.77 min, M+H+=423

Provenance & Evidence