Dimethylamine → rac-(2'S,3'R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluoro-phenyl)-2'-(2,2-dimethyl-propyl)-2-oxo-1,2-dihydro-spiro[indole-3,3'-pyrrolidine]-5'-carboxylic acid (4-dimethylcarbamoyl-phenyl)-amide

Participants

Reaction Steps

In a manner similar to the method described in Example 22, rac-4-{[(2′S,3′R,4′S,5′R)-6-chloro-4′-(3-chloro-2-fluoro-phenyl)-2′-(2,2-dimethyl-propyl)-2-oxo-1,2-dihydro-spiro[indole-3,3′-pyrrolidine]-5′-carbonyl]amino}-benzoic acid (30 mg, 0.051 mmol) was reacted with EDCI (19 mg, 0.1 mmol), HOBt (14 mg, 0.1 mmol), and dimethylamine (0.1 mL, O2 mmol) at 60° C. to give rac-(2′S,3′R,4′S,5′R)-6-chloro-4′-(3-chloro-2-fluoro-phenyl)-2′-(2,2-dimethyl-propyl)-2-oxo-1,2-dihydro-spiro[indole-3,3′-pyrrolidine]-5′-carboxylic acid (4-dimethylcarbamoyl-phenyl)-amide as a light yellow solid (Yield, 10 mg, 32%).

Provenance & Evidence