1,2-Dichloroethane → HCID 69936460, compound

Participants

Reaction Steps

Neat 1-methyl-1H-pyrazol-4-amine (38.2 mg, 0.39 mmol) was added in one charge to a stirred solution of 2-[(phenylmethyl)oxy]-5-(4-pyridinyl)benzoic acid (may be prepared as described in Description 79; 100 mg, 0.33 mmol), EDC (188 mg, 0.98 mmol) and HOBT (150 mg, 0.983 mmol) in dimethylformamide (3 ml) in air at room temperature. The reaction mixture was stirred at room temperature overnight. Water (20 ml) was added, and the mixture was extracted with ethyl acetate (20 ml×2). The organic phase was dried over Na2SO4, and concentrated in vacuo to give crude product, which was purified by prep-HPLC (Gilson GX-281; waters X-Bridge 5 μm 30*100 mm; A: 0.1M NH3.H2O/Water; B: CH3CN) twice to yield the title compound as a white solid. 58 mg.

Provenance & Evidence