Hydrochloric Acid → HCID 122436167, compound

Participants

Reaction Steps

A 4M solution of HCl in 1,4-dioxane (1.06 mL; 4.22 mmol; 25 eq.) was added to a solution of 3-[2-(6-chloro-5,7-dimethyl-1H,3H-2,4,7a,8-tetraaza-cyclopenta[a]indene-2-carbonyl)-phenoxy]-3-trifluoromethyl-pyrrolidine-1-carboxylic acid tert-butyl ester (98 mg; 0.17 mmol; 1 eq.) in 1,4-dioxane (10 mL) and the resulting mixture was stirred at room temperature for 20 hours then concentrated in vacuo. The residue was partitioned between DCM and sat. aq. NaHCO3 and the aqueous layer was extracted with DCM. The combined organic phase was washed with brine, dried over magnesium sulfate and concentrated in vacuo. Purification by mass directed preparative HPLC afforded the title compound (15 mg, 25%) as a white solid. HPLC (max plot) 95.9%, Rt 3.23 min. UPLC/MS: (MS+) 480.3 ([M+H]+).

Provenance & Evidence