Triethylamine → (3R)-3-(4-Cyanobenzyl)-1-(3,5-dichlorophenyl)-3-methyl-2-oxo-N-(1-{[2-(2H-tetrazol-5-yl)ethyl]carbamoyl}cyclopropyl)-2,3-dihydro-1H-imidazo[1,2-a]imidazole-5-carboxamide

Participants

Reaction Conditions

Reaction Steps

1-{[(R)-5-(4-Cyano-benzyl)-7-(3,5-dichloro-phenyl)-5-methyl-6-oxo-6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carbonyl]-amino}-cyclopropanecarboxylic acid (50 mg, 0.09 mmol) and HATU (57 mg, 0.15 mmol), were combined with a heterogeneous solution of 2-(1H-tetrazol-5-yl)-ethylamine formiate (45 mg, 0.26 mmol) in anhydrous DMF (1 mL) and cooled to 0° C. Et3N (0.043 mL, 0.3 mmol) was added to the reaction. After 18 h the reaction slowly warmed to room temperature. The crude reaction solution was filtered and purified via reverse HPLC to yield 45 mg of the title compound as a white solid, m/z 619.5 [M+1]+).

Provenance & Evidence