1,2-Dichloroethane → HCID 44599238, compound

Participants

Reaction Steps

A mixture of (2S)-2-(3-fluoro-benzyl)-pyrrolidine-1,2-dicarboxylic acid 1-tert-butyl ester (97.0 mg, 0.3 mmol), 1-cyclobutyl-[1,4]diazepane hydrochloride (75.0 mg, 0.3 mmol), HOBt (49.0 mg, 0.36 mmol), EDC (69.2 mg, 0.36 mmol) and N-methylmorpholine (98.0 mg, 0.96 mmol) in CH2Cl2 (10 mL) was stirred at rt for 18 h. The reaction mixture was diluted with CH2Cl2, washed successively with 1 N NaOH and water, dried, and concentrated. The residue (210 mg) was purified by FCC to provide the title compound (47.0 mg, 34%). MS (ESI): mass calcd. for C26H38FN3O3, 459.60; m/z found, 460.2 [M+H]+. 1H NMR (CDCl3): 7.25-7.18 (m, 1H), 6.99-6.83 (m, 3H), 3.61-3.48 (m, 2H), 3.37-3.10 (m, 4H), 2.92-2.52 (m, 3H), 2.49-2.25 (m, 2H), 2.23-1.80 (m, 9H), 1.76-1.55 (m, 5H), 1.51-1.48 (m, 9H).

Provenance & Evidence