Hydrochloric Acid → [4-Azidomethyl-1-hydroxy-6-(pyrazin-2-yloxy)-1,3-dihydro-benzo[c][1,2]oxaborol-3-yl]-acetic acid ethyl ester

Participants

Reaction Conditions

Reaction Steps

To a mixture of (4-azidomethyl-1,6-dihydroxy-1,3-dihydro-benzo[c][1,2]oxaborol-3-yl)-acetic acid ethyl ester (550 mg, 1.89 mmol), 2-chloropyrazine (350 mg, 3.05 mmol), Cs2CO3 (1.34 g, 4.11 mmol) in 5 mL of DMF was heated to 80° C. for 3.5 h. The reaction mixture was adjusted to pH 3 by 1N HCl. The crude product was purified by HPLC to yield 200 mg of the title compound.

Provenance & Evidence