反应详情

0.1 g (0.37 mmol) of methyl 2-cyano-3-[(3-fluorophenyl)amino]-3-(methylsulfanyl)-2-propenoate and 0.06 g (0.41 mmol) of 2-cyclopentylethanamidine hydrochloride are dissolved in 1 ml of DMF and heated with 0.11 g (0.82 mmol) of potassium carbonate at 90° C. overnight. After filtration, the solvent is removed in vacuo and the residue is purified by preparative HPLC (YMC Gel ODS-AQ S 5/15 μm; eluent A: water, eluent B: acetonitrile; gradient: 0 min 30% B, 5 min 30% B, 50 min 95% B) purified. 70 mg (59% of theory) of the product are obtained as a colorless solid.

1. filtrationAfter filtration
2. customthe solvent is removed in vacuo
3. customthe residue is purified by preparative HPLC (YMC Gel ODS-AQ S 5/15 μm; eluent A: water, eluent B: acetonitrile; gradient: 0 min 30% B, 5 min 30% B, 50 min 95% B)
4. custompurified
5. custom70 mg (59% of theory) of the product are obtained as a colorless solid