1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → HCID 58788458, compound

Participants

Reaction Steps

HOBT (209 mg, 1.55 mmol), 5-chloroindole-2-carboxylic acid (303 mg, 1.55 mmol), DIPEA (0.27 mL, 1.55 mmol) and then EDCI (370 mg, 1.94 mmol) were added to a solution of 3-amino-1-{[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}-3,4-dihydroquinolin-2(1H)-one (Method 8, 428 mg, 1.55 mmol) in DCM (10 mL). The reaction was stirred for 18 h at ambient temperature, diluted with EtOAc (20 mL), washed with 1 N NaOH (15 mL), 0.1 N HCl (15 mL), saturated aqueous NaHCO3 solution (15 mL), dried (Na2SO4) and the volatiles removed under reduced pressure to give the title compound (684 mg, 97%) as a pale yellow solid.

Provenance & Evidence