Cesium carbonate → HCID 70981270, compound

Participants

Reaction Conditions

Reaction Steps

(4-Chloro-benzyl)-(6-chloro-3-nitro-pyridin-2-yl)-amine (685 mg, 2.31 mmol), ((S)-1-carbamoyl-ethyl)-methyl-carbamic acid tert-butyl ester (Intermediate A1) (606 mg, 3.0 mmol), Pd2 dba3 (210 mg, 0.23 mmol), BINAP (286 mg, 0.46 mmol) and Cs2CO3 (1.5 g, 4.62 mmol) were added to 1,4-dioxane (15 mL). The mixture was evacuated and flushed with N2 three times and then heated at 90° C. for 2 hours. The mixture was cooled, diluted with EtOAc, filtered and concentrated in vacuo. The residue was purified by SiO2 chromatography (10-30% EtOAc/Petrol) to give {1-[6-(4-chloro-benzylamino)-5-nitro-pyridin-2-ylcarbamoyl]-ethyl}-methyl-carbamic acid tert-butyl ester (611 mg) as an orange foamy solid. MS: [M+H]+=464.

Provenance & Evidence