1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → HCID 117729238, compound

Participants

Reaction Steps

A solution of Intermediate 38a (5.95 g, 34.2 mmol) in DCM (60 mL) was treated with EDCI (7.87 g, 34.2 mmol), HOBt (0.462 g, 41.0 mmol) and (5-fluoro-pyridin-2-yl)-hydrazine (4.35g g, 34.2 mmol) and the solution was stirred at RT for 16 hours. The reaction mixture was partitioned between H2O (50 mL) and DCM (40 mL) and the phases were separated. The organic phase was washed with sat. bicarbonate solution and the brine. The volatiles were concentrated in vacuo and the resultant residue was purified by FCC using 0-10% MeOH in DCM to afford the title compound (1.74 g, 20%). LCMS (Method 3): Rt 0.44 min, m/z 282 [MH+].

Provenance & Evidence