1-Hydroxybenzotriazole → HCID 58739163, compound

Participants

Reaction Steps

A mixture of (S)-2-tert-butoxycarbonylamino-propionic acid (0.083 mmol), (S)-1-(3-pyridin-3-yl-phenyl)-ethylamine (12.7 mg, 0.064 mmol), EDAC.HCl (18.4 mg, 0.096 mmol), HOBT (13 mg, 0.096 mmol and d iisopropylethylamine (33 μL, 0.192 mmol) ) in DMF (2 mL) was stirred at room temperature for 18 h. The reaction mixture was purified by preparative HPLC (Primeshere C18-HC 21.2×100 mm; (5 mM NH4OAc ) 0–100% gradient over 5 min; 20 mL/min flow rate). The solvents were removed through evaporation on the speed-vac, and the crude product was dissolved in CH2Cl2/TFA (1: 1, 2 mL) and stirred at room temperature for 3 h. The reaction mixture was concentrated on the speed-vac and purified by preparative HPLC (5 mM NH4OAc buffer; gradient 0% to 100% B in 10 min (A: 10% CH3CN/H2O; B: 90% CH3CN/H2O; column: Primesphere C18 HC 21.2×100 mm) to afford the title product.

Provenance & Evidence