Trifluoroacetic acid → 2(R)-[2,2-difluoro-1(S)-(4-fluorophenyl)-2-(4-methylsulfanyl-phenoxy)ethylamino]-3-mercaptopropionic acid

Participants

Reaction Steps

To a solution of 2(R)-[2,2-difluoro-1(S)-(4-fluorophenyl)-2-(4-methylsulfanylphenoxy)-ethylamino]-3-tritylsulfanylpropionic acid (0.69 g, 1.04 mmol) in DCM (0.8 ml), TFA (0.322 ml, 4.18 mmol) and triethylsilane (0.332 ml) were added. After stirring 3 h, solvent and excess of TFA were evaporated under vacuum. The residue was dissolved in benzene and evaporated again on rotary evaporator to give 2(R)-[2,2-difluoro-1(S)-(4-fluorophenyl)-2-(4-methylsulfanyl-phenoxy)ethylamino]-3-mercaptopropionic acid. The residue was dissolved in 1N NaOH (4 ml) and the solution was used immediately in the next step.

Provenance & Evidence