Chloroform → HCID 178518305, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 4-{[4-(2-Hydroxymethyl-pyrrolidin-1-ylmethyl)-phenylamino]-methylene}-6-iodo-4H-isoquinoline-1,3-dione (200 mg, 0.40 mmol) in N,N-dimethylformamide (10 mL) were added 3-thienylboronic acid (120 mg, 0.94 mmol) and Na2CO3 (216 mg, 2.0 mmol). Pd2(dba)3.CHCl3 (20 mg, 0.02 mmol) and P(tBu)3.HBF4 (19 mg, 0.06 mmol) were then added. The mixture is then degassed and heated at 100° C. for 1 h. The N,N-dimethylformamide is then evaporated under reduced pressure and the residue is taken up in EtOAc and H2O. The EtOAc layer is dried and evaporated. The residue, which resulted, is subjected to chromatography to provide the desired product (90 mg, 49%). MS (ESI): 460.2 (M+1)+1

Provenance & Evidence