1,2-Dichloroethane → HCID 70652350, compound

Participants

Reaction Steps

2-((R)-3-(tert-Butoxycarbonylamino)piperidin-1-yl)-2-(2-fluorophenyl)acetic acid (174 mg, 0.494 mmol), ammonium chloride (79 mg, 1.481 mmol), DIPEA (0.431 mL, 2.469 mmol), EDC (142 mg, 0.741 mmol) and HOBT (113 mg, 0.741 mmol) were stirred in DMF (5 mL) at room temperature for 3 days. Saturated NaHCO3 was added and the products extracted into EtOAc (×2). The combined organic extracts were washed with brine, dried over Na2SO4, filtered and concentrated in vacuo. Purification of the residue by MPLC (12-100% EtOAc-hexanes) gave tert-butyl (3R)-1-(2-amino-1-(2-fluorophenyl)-2-oxoethyl)piperidin-3-ylcarbamate as a mixture of diastereoisomers.

Provenance & Evidence