1,1,1-Trifluoro-3-iodopropane → N-{[(2S)-5-Fluoro-7-(methylsulfonyl)-2,3-dihydro-1,4-benzodioxin-2-YL]methyl}-N-(3,3,3-trifluoropropyl)amine

関与物質

反応条件

反応手順

A mixture of 1-[(2S)-5-fluoro-7-(methylsulfonyl)-2,3-dihydro-1,4-benzodioxin-2-yl]methaneamine (0.3 g, 1.1 mmol), 1,1,1-trifluoro-3-iodopropane (0.16 ml, 1.4 mmol) K2CO3 (0.32 g, 2.3 mmol) and ACN (4 ml) was heated under microwave radiation at 120° C. for 30 min. The mixture was filtrated and evaporated to dryness and the product was purified by flash column chromatography (EtOAc). Yield: 0.12 g, 31%. The amine was converted to the hydrochloric acid salt and crystallized from MeOH/Et2O. M.p. 233° C. MS m/z (rel. intensity, 70 eV) 357 (M+, 1), 274 (3), 127 (5), 126 (bp), 69 (3). [α]=−53° (MeOH).

情報源と証拠