Toluene → HCID 10255967, compound

Participants

Reaction Conditions

Reaction Steps

To a dry flask was charged the product from example 22 part (ii) (1 g), N-tert-Butoxycarbonylpiperazine (0.48 g), Pd2(dba)3 (3 mg), 2,2′-bis(diphenylphosphino)-1,1′-binapthyl Binap (10 mg) and toluene (5 ml). The reaction was heated to 110° C. for 1 hour then allowed to cool. The mixture was diluted with EtOAc, washed with water, dried over MgSO4 and concentrated in vacuo. The residue was purified using Flash column chromatography (eluent 25% EtOAc/Hexane then 50% EtOAc/Hexane/1% Acetic acid). Further purification using reverse phase preparative HPLC (eluent MeCN/NH3 (aq)) gave titled compound (0.021 g).

Provenance & Evidence