1-Hydroxybenzotriazole → HCID 15601613, compound

Participants

Reaction Steps

Boc-Phe-OH (79.6 g, 0.3 mole), Gly-OBzl-TosOH (111 g, 1.1 eq), and HOBt (44.6 g, 1.1 eq) were dissolved in DMF (300 ml). WSCI (60.4 ml, 1.1 eq ) was added dropwise while cooling, and the solution was stirred overnight. DMF was distilled off. The residue was dissolved in CHCl3, and the solution was washed with 5% NaHCO3, 10% Na2CO3, water, 1HCl, and water, in order, and dried over MgSO4. The CHCl3 was distilled off, and to the residue, Et2O was added. The thus-produced powder was obtained by filtration and recrystalized two times with AcOEt/Et2O to obtain the object product (59 g).

Provenance & Evidence