Hydrochloric Acid → HCID 71610220, compound

Participants

Reaction Steps

HCl (1.3 mL) was added to a solution of (R)-3-[2-(6-chloro-5,7-dimethyl-1H,3H-2,4,7a,8-tetraaza-cyclopenta[a]indene-2-carbonyl)-5-fluoro-phenoxy]-pyrrolidine-1-carboxylic acid tert-butyl ester (700 mg; 1.32 mmol; 1 eq.) in 1,4-dioxane (10 mL) was stirred at room temperature for 16 hours then concentrated in vacuo. The reaction mixture was diluted with DCM, washed with 0.1M NaOH, dried over magnesium sulfate and concentrated in vacuo to afford the title compound (550 mg, 97%) as yellow foam. 1H NMR (DMSO-d6) δ 7.40-7.31 (m, 1H), 7.09-7.01 (m, 1H), 6.93-6.83 (m, 1H), 5.03-4.93 (m, 1H), 4.86-4.76 (m, 2H), 4.62-4.43 (m, 2H), 3.13-3.02 (m, 1H), 2.84 (s, 1.5H), 2.81 (s, 1.5H), 2.78-2.69 (m, 2H), 2.62 (s, 1.5H), 2.57 (s, 1.5H), 2.07-1.89 (m, 1H), 1.79-1.61 (m, 2H). HPLC (max plot) 97.2%, Rt 2.74 min. UPLC/MS: (MS+) 430.4 ([M+H]+).

Provenance & Evidence