1,2-Dichloroethane → HCID 12096227, compound

Participants

Reaction Steps

To a stirred solution of 4-(1-(2-hydroxy-2-methylpropyl)-cis-3-phenylpyrrolidin-4-yl)-6-methyl-1-carboxymethyl-2-pyridinone from step 8 above (0.23 mmol), 5-aminomethyl-3-fluoro-7-azaindole bis hydrochloride (55 mg, 0.23 mmol), HOBT (35 mg, 0.23 mmol) and DIEA (0.12 mL, 0.69 mmol) in DMF (2 mL) was added EDC (134 mg, 0.46 mmol). The resulting solution was stirred at ambient temperature for 18 h. The solvent was removed in vacuo and the residue was purified by flash column chromatography using a gradient elution of 96:4 to 92:8 CH2Cl2:MeOH as eluant to give the title compound as an amorphous solid (0.1 g, TLC Rf=0.4, 92:8 CH2Cl2:MeOH; HPLC RT=4.71 min, method A).

Provenance & Evidence