Cesium carbonate → HCID 118223446, compound

Participants

Reaction Steps

Mix the compound obtained in Step 2 (610 mg, 1.9 mmol), cyclopropanecarboxamide (193 mg, 2.27 mmol), (±)-2,2′-bis(diphenylphosphino)-1,1′-binaphthalene (BINAP, 118 mg, 0.19 mmol), Cs2CO3 (1.238 g, 3.8 mmol) and tris(dibenzylideneacetone)dipalladium [Pd2(dba)3, 122 mg, 0.133 mmol] in 1,4-dioxane (30 mL). Stir the reaction at 120° C. under N2 for 16 hrs. Cool the reaction, filter, concentrate the filtrate under reduced pressure to give the crude product. Purification by chromatography (silica gel, EtOAc:PE=1:1) affords the title compound (500 mg, 70.8%). MS: (M+1): 372.2.

Provenance & Evidence