1,2-Dichloroethane → tert-butyl 4-(2-chloroisonicotinoyl)tetrahydro-1(2H)-pyrazinecarboxylate

Participants

Reaction Steps

2-Chloroisonicotinic acid (12-2, 250 mg, 1.59 mmole), tert-butylpiperazine-1-carboxylate (355 mg, 1.9 mmole), EDC (365 mg, 1.9 mmole), and HOBt (257 mg, 1.9 mmole) were combined in dry DMF (10 mL). To this was added Et3N (0.55 mL, 3.97 mmole) at RT. After 18 hr the mixture was diluted with H2O and extracted with EtOAc (4×). The combined organic layers were washed with H2O, brine; then dried (MgSO4), filtered, and concentrated to give the titled compound as an amber oil which was used immediately in the next step.

Provenance & Evidence