1,2-Dichloroethane → HCID 178507937, compound

Participants

Reaction Steps

A mixture of 4-(2,6-difluorobenzylamino)-1H-pyrazole-3-carboxylic acid (1.0 g, 3.7 mmol) (Example 16D), 2,3-diaminobenzylalcohol (560 mg, 4.1 mmol), EDC (870 mg, 4.5 mmol) and HOBt (610 mg, 4.5 mmol) in DMF (20 ml) was stirred at ambient temperature for 18 h and then reduced in vacuo. The residue was partitioned between EtOAc and brine and the organic portion dried (MgSO4) and reduced in vacuo. The residue was purified by flash column chromatography [SiO2, EtOAc-hexane (1:1, 2:1)] to give 4-(2,6-difluoro-benzoylamino)-1H-pyrazole-3-carboxylic acid (2-amino-3-hydroxymethyl-phenyl)-amide (860 mg).

Provenance & Evidence