反应详情

A mixture of 200 mg (0.604 mmol) N-{2-(2-cyano-3-oxobut-1-en-1-yl)furo[3,2-c]pyridin-4-yl}-benzamide (Example 4A) and 329 mg (2.41 mmol) (2E)-3-amino-4,4,4-trifluorobut-2-enenitrile [CAS Reg.-No. 33561-24-9; prepared following A. W. Lutz, U.S. Pat. No. 3,635,977 and also C. G. Krespan, J. Org. Chem. 34, 42-45 (1969)] in 2-propanol (1 ml) was stirred at reflux for 12 h. Upon cooling, the mixture was concentrated under reduced pressure, and the residue was directly purified by preparative RP-HPLC (acetonitrile/water+0.1% TFA gradient, final mixture 90:10 v/v) to yield 171 mg (63% of th.) of the racemic title compound.

1. customprepared following A
2. temperatureat reflux for 12 h
3. temperatureUpon cooling
4. concentrationthe mixture was concentrated under reduced pressure
5. customthe residue was directly purified by preparative RP-HPLC (acetonitrile/water+0.1% TFA gradient, final mixture 90:10 v/v)