3-Isoxazolamine → [2-(2-Isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen-8-ylmethyl]-isoxazol-3-yl-amine

Participants

Reaction Steps

Following the procedure for 119, 2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene-8-carbaldehyde and 3-amino-isoxazole were reacted. Purification by flash chromatography (SiO2, 0-20% EtOAc in DCM) gave 284 as a white solid (154 mg, 52%). LCMS: RT=10.79 min, [M+H]+=409. 1H NMR δ (ppm) (CDCl3): 8.33 (1 H, d, J=8.10 Hz), 8.04 (1 H, d, J=1.68 Hz), 7.90 (1 H, s), 7.16 (1 H, d, J=8.19 Hz), 7.06 (1 H, s), 5.93-5.84 (1 H, m), 5.85-5.83 (1 H, m), 4.42 (2 H, s), 4.38 (2 H, t, J=5.02 Hz), 3.42-3.36 (2 H, m), 1.60 (6 H, d, J=6.62 Hz). 1 Exchangeable proton not seen.

Provenance & Evidence