Ethanol → tert-butyl N-[4-[[5-(2-methylphenyl)-3-pyridinyl]sulfonyl]-5-methylsulfanylthiophene-2-carboximidoyl]carbamate

Participants

Reaction Conditions

Reaction Steps

The procedure described in Example 1: step c was followed using {[4-(5-Bromo-pyridine-3-sulfonyl)-5-methylsulfanyl-thiophen-2-yl]-imino-methyl}-carbamic acid tert-butyl ester (50 mg, 0.08 mmol), 2-methyl phenyl boronic acid (23 mg, 0.17 mmol), Pd(PPh3)4 (19 mg, 0.02 mmol), aqueous Na2CO3 (2M, 800 μL, 0.4 mmol), ethanol (800 μL) and toluene (1600 μL). The reaction was heated to 80° C. for 12 hours. The residue was dissolved into EtOAc and washed with brine. The organic layers were dried (MgSO4) and removal of the solvents in vacuo resulted in a crude mixture of the product that was used without further purification or characterization.

Provenance & Evidence