3-Oxabicyclo(3.1.0)hexane-2,4-dione → cis-2-{[1-(2-Fluorobenzyl)-7-(2-{[(1-methyl-1H-imidazol-4-yl)sulfonyl]amino}ethoxy)-1,2,3,4-tetrahydronaphthalen-2-yl]carbamoyl}cyclopropanecarboxylic acid

Participants

Reaction Conditions

Reaction Steps

cis-N-(2-{[7-Amino-8-(2-fluorobenzyl)-5,6,7,8-tetrahydronaphthalen-2-yl]oxy}ethyl)-1-methyl-1H-imidazole-4-sulfonamide (50 mg, 0.109 mmol) was dissolved in dimethylformamide (2 mL), 3-oxabicyclo[3.1.0]hexane-2,4-dione (13.4 mg 0.12 mmol) was added and the reaction mixture was heated to 110° C. for 2 h. The solvent was removed in vacuo and the crude product was taken up in dichloromethane and washed successively with water (2×) and saturated sodium chloride solution (1×) and dried (magnesium sulfate). The solvent was evaporated in vacuo and the crude product was used for the next step without further purification. Yield: 63 mg (colorless foam).

Provenance & Evidence