Diisopropylethylamine → (2S,4R)-tert-butyl 4-cyano-2-(4-(4-fluorophenoxy)phenylcarbamoyl)pyrrolidine-1-carboxylate

関与物質

反応手順

Step (a) A flask was charged with (2S,4R)-1-(tert-butoxycarbonyl)-4-cyanopyrrolidine-2-carboxylic acid (1.0 g, 4.16 mmol), HATU (1.74 g, 4.58 mmol), 4-(4-fluorophenoxy)aniline (0.844 g, 4.16 mmol), DIEA (4.8 mL, 27 mmol) and DMF (10 mL). The reaction mixture was stirred at ambient temperature for 30 minutes and then quenched with saturated sodium bicarbonate (aq., 20 mL). The mixture was extracted with ethyl acetate (60 mL) and the extract was washed with deionized water (30 mL), and then brine (30 mL), dried over anhydrous sodium sulfate, filtered, and concentrated to give (2S,4R)-tert-butyl 4-cyano-2-(4-(4-fluorophenoxy)phenylcarbamoyl)pyrrolidine-1-carboxylate. The crude mixture was used without further purification.

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