1,2-Dichloroethane → HCID 66611615, compound

Participants

Reaction Steps

To a solution of 5-(benzyloxy)-4-((benzyloxy)carbonyl)-2-chlorobenzoic acid (may be prepared as described in D74) (500 mg, 1.260 mmol) in N,N-Dimethylformamide (DMF) (5 mL) were added DIPEA (0.660 mL, 3.78 mmol), 1-methylpiperazine (0.182 mL, 1.638 mmol), 1-hydroxy-7-azabenzotriazole (206 mg, 1.512 mmol) and EDC (435 mg, 2.268 mmol). The mixture was stirred at room temperature for 8 hrs. The solvent was removed in vacuo. The residue was redissolved in DCM (10 mL) and washed with water (10 mL), dried over MgSO4 and concentrated in vacuo. Purification by column (Si, Isolute, 10% 2M NH3 in MeOH/DCM) gave the title product as a yellow solid (400 mg, 66% yield).

Provenance & Evidence