1,2-Dichloroethane → HCID 178453836, compound

Participants

Reaction Steps

A mixture of Example 213a (3.950 g, 11.23 mmol), 2-(tert-butoxycarbonylamino)acetic acid (2.165 g, 12.36 mmol), HOBT (1.892 g, 12.36 mmol), EDC (2.369 g, 12.36 mmol), and triethylamine (2.04 mL, 14.6 mmol) in tetrahydrofuran (100 mL) was stirred at room temperature for 3 hours. The reaction was diluted with 50% brine and extracted with EtOAc (2×). The combined organic layers were dried over MgSO4, filtered, and concentrated. The residue was triturated with EtOAc/hexane (8:2) to give 2.756 g of the title compound. The filtrate was purified on an 80 g column using the ISCO Companion flash system eluting with EtOAc/hexane (7:3 to 8:2) to give the 1.091 g more title compound.

Provenance & Evidence