1,2-Dichloroethane → HCID 69421498, compound

Participants

Reaction Steps

To a stirred solution of (βS)-N-(tert-butoxycarbonyl)4-fluoro-β-methyl-L-phenylalanine Example 1, Step E, 0.15 g, 0.51 mmol) in anhydrous DMF (2 mL) was added EDC (0.25 g, 1.33 mmol), HOBT (0.18 g, 1.33 mmol), (3S)-3-fluoropyrrolidine hydrochloride (0.18 g, 1.45 mmol) and N,N′-diisopropylethylamine (0.23 mL, 1.31 mmol). After stirring at room temperature for 12 h, the reaction was diluted with ethyl acetate. The organic phase was washed sequentially with brine, 1N hydrochloric acid and 1N aqueous sodium hydroxide solution, dried over sodium sulfate, and evaporated in vacuo to yield the crude coupled product, which was used directly for the next step.

Provenance & Evidence