Hydrazine → tert-butyl((1S)-3-hydrazino-1-(4-(trifluoromethyl)benzyl)propyl)carbamate

Participants

Reaction Steps

(R)-tert-Butyl 2-(4-(trifluoromethyl)benzyl)-5-oxopyrrolidine-1-carboxylate (1.46 g, 4 mmol) (prepared as shown in Scheme 15) was treated with hydrazine (0.5 mL, 16 mmol) at 50° C. in THF for 30 minutes. The mixture was partitioned between EtOAc and saturated aqueous ammonium chloride, and dried over sodium sulfate. Evaporation provided the desired product as a white amorphous solid (1.27 g, 87%). LCMS (API-ES) m/z: 276 (M-Boc+H+).

Provenance & Evidence