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General Procedure A solution of amine 2a-i (5 mmol) in dried CH2Cl2 (2,5 mL) was heated until reflux. After a period of 15 min ethyl N-(cyanomethyl)formimidate 1 (5 mmol, 560 mg) was added under N2 counterflow. The mixture was allowed to stir under reflux for 2 h. To the hot reaction mixture the 1,3-biselectrophile of type 4a-e (5 mmol) was added. The mixture was stirred for 8 h. Then it was cooled down to ambient temperature. The crude product was worked up through flash column chromatography to obtain the product as white needles. Selected Data for 5o 1H NMR (400 MHz, CDCl3, δ, 3.79 (s, 3 H, OCH3, 5.47 (s, 2 H, CH2, 6.89 (m, 2 H, Ph, 7.33 (m, 2 H, Ph, 7.87 (s, 1 H, H-6, 8.31 (s, 1 H, H-2, 13C NMR (100 MHz, CDCl3, δ, 47.5 (OCH3, 55.3 (CH2, 111.5 (m, C-6, 122.3 q, 1JCF, 278 Hz, CF3
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3): δ = -62.59, -66.55.
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33
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0042243695
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