Hydrochloric Acid → HCID 86697001, compound

Participants

Reaction Steps

In a sealed 20 ml microwave vial, a solution of compound 52 (340 mg, 1.01 mmol), KOAc (297 mg, 3.02 mmol) and Pd(PtBu3)2 (52.7 mg, 0.101 mmol) in MeOH (5 mL) was heated in the microwave for 45 min at 100° C. Diluted with EtOAc, washed with water and brine, dried (MgSO4), filtered and concentrated under vacuum. The residue was dissolved in DCM (2.50 mL) then 4 N HCl in dioxane (2.52 mL, 10.1 mmol) was added. The reaction was stirred at room temperature and concentrated under vacuum to give compound 178 (196 mg, quantitative) as a solid. 1H NMR (400 MHz, DMSO-d6) δ 9.46 (br. s., 2 H), 6.92 (s, 1 H), 4.15 (s, 2 H), 4.00 (s, 3 H), 2.58 (s, 3 H).

Provenance & Evidence