1-(2-Morpholinoethyl)-1H-pyrazole-4-boronic acid pinacol ester → 9-[1-(2-Morpholin-4-yl-ethyl)-1H-pyrazol-4-yl]-2-[2-(2,2,2-trifluoro-ethyl)-2H-[1,2,4]triazol-3-yl]-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene

Participants

Reaction Steps

8-Bromo-2-[2-(2,2,2-trifluoro-ethyl)-2H-[1,2,4]triazol-3-yl]-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene and 4-(2-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)ethyl)morpholine were reacted under palladium Suzuki conditions to give 115 (17% yield). LC/MS (ESI+): m/z 532 (M+H). 1H NMR (400 MHz, DMSO) δ 8.48 (d, J=2.1, OH), 8.30 (s, OH), 8.07 (s, OH), 7.76 (s, OH), 7.49 (dd, J=8.3, 2.2, OH), 7.09 (d, J=8.3, OH), 5.89 (q, J=8.6, OH), 4.38 (t, J=4.9, OH), 4.25 (t, J=6.6, OH), 3.61-3.51 (m, 1H), 3.48 (t, J=4.9, OH), 2.75 (t, J=6.6, OH), 2.45-2.35 (m, 1H)

Provenance & Evidence