Methanesulfonyl chloride → HCID 58204033, compound

Participants

Reaction Steps

Following the procedure for 395, 8-azetidin-3-yl-2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene hydrochloride salt and methanesulfonyl chloride were reacted. The reaction mixture was loaded directly onto a silica column with no aqueous work-up to give 259 isolated as a white solid (67 mg, 84%). LCMS: RT=10.97 min, [M+H]+=446. 1H NMR δ (ppm) (CDCl3): 8.36 (1 H, d, J=8.20 Hz), 7.90 (1 H, d, J=0.68 Hz), 7.16 (1 H, dd, J=8.24, 1.88 Hz), 7.02 (1 H, d, J=1.85 Hz), 5.93-5.83 (1 H, m), 4.42-4.36 (2 H, m), 4.30-4.22 (2 H, m), 4.10-4.03 (2 H, m), 3.83-3.73 (1 H, m), 3.43-3.37 (2 H, m), 2.90 (3 H, s), 1.61 (6 H, d, J=6.63 Hz)

Provenance & Evidence