5-Amino-1-cyclopropyl-6,7,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid → HCID 70284622, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 5-amino-1-cyclopropyl-6,7,8-trifluoro-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid (63 mg, 0.21 mmol), trans-3-hydroxy-4-(1,2,3-triazol-1-yl)-pyrrolidine hydrochloride (100 mg, 0.52 mmol) and diazabicycloundecane (79 mg, 0.52 mmol) in pyridine was heated at 110° C. for 20 h. The reaction mixture was concentrated and the residue was triturated with water. The separated solid was filtered, washed with water and acetonitrile and dried under vacuum at 40° C. Yield: 35 mg (40%), m.p. 261°-165.5° C. 1H NMR (TFA) δ: 1.33-1.51 (m, 4H), 4.24 (m, 2H), 4.60 (m, 2H), 4.92 (m, 1H), 5.20 (m, 1H), 5.79 (m, 1H), 8.59 (d, 1H), 8.78 (s, 1H), 9.15 (s, 1H).

Provenance & Evidence