Potassium tert-butoxide → 4-(4-Cyano-2-methoxyphenyl)-6-methyl-5-(4-methyl-1,3-thiazol-2-yl)-2-(trifluoromethyl)-1,4-di-hydropyridine-3-carbonitrile

Participants

Reaction Steps

100 mg (0.335 mmol) of the compound from example 6A, 46 mg (0.335 mmol) of 3-amino-4,4,4-tri-fluorobut-2-enenitrile [preparation in analogy to U.S. Pat. No. 3,635,977 and K. Krespan, J. Org. Chem. 34, 42-45 (1969)] and 5.6 mg (0.05 mmol) of potassium tert-butoxide are dissolved in 4 ml of isopropanol and stirred at the reflux temperature overnight. After cooling to room temperature, the volatile components are removed in a rotary evaporator, and the crude product is purified by preparative HPLC (eluent: acetonitrile/water with 0.1% formic acid, gradient 20:80→95:5). 119 mg (82% of theory) of the title compound are obtained.

Provenance & Evidence