1,1'-Carbonyldiimidazole → (2S,4S)-4-(8-chloro-2-(4-isopropylthiazol-2-yl)-7-methoxyquinolin-4-yloxy)-N-(hex-5-enyl)-1-(1H-imidazole-1-carbonyl)-N-methylpyrrolidine-2-carboxamide

Participants

Reaction Steps

Compound 135 (10 g) was dissolved in anhydrous dichloromethane (20 mL) under argon. 1,1′-Carbonyldiimidazole (2 eq.) was added at room temperature. The reaction mixture was stirred for 45 min. The mixture was diluted with DCM, washed with water, dried over Na2SO4, and concentrated under vacuum. Compound 136 (9.9 g) was recovered as an off-white foam in 99% yield and in 98% purity (HPLC).

Provenance & Evidence