Sodium Hydroxide → HCID 68453838, compound

Participants

Reaction Steps

3-[4-tert-Butyl-2-(2-methoxyethoxy)phenyl]acrylic acid ethyl ester (40.4 mg, 0.132 mmol, 1 eq) and sodium hydroxide (52.8 mg, 1.32 mmole, 10 eq) were added in methanol and H2O. The reaction mixture was purified according to step 2 of Example 22 to give 3-[4-tert-Butyl-2-(2-methoxyethoxy)phenyl]acrylic acid (36.5 mg, 77.3%). 3-[4-tert-Butyl-2-(2-methoxyethoxy)-phenyl]acrylic acid (26.4 mg, 0.095 mmol, 1 eq.), Diethylcyanophosphine (17.3 μl, 0.114 mmol, 1.2 eq), N-(4-Aminomethyl-2-fluoro-6-vinylphenyl)methanesulfonamide (40.8 mg, 0.1114 mol, 1.2 eq.), and Triethylamine (39.7 μl, 0.285 mmol, 3 eq) were added in DMF. The mixture was stirred for overnight at room temperature. The reaction mixture was purified according to Example 17 to give a whitish solid (28.4 mg, 59.2%).

Provenance & Evidence