1,1'-Carbonyldiimidazole → (2S,4S)-N-(hex-5-enyl)-1-(1H-imidazole-1-carbonyl)-4-(7-methoxy-8-methyl-2-(4-(trifluoromethyl)thiazol-2-yl)quinolin-4-yloxy)-N-methylpyrrolidine-2-carboxamide

Participants

Reaction Steps

Compound 127 (18.35 g) was dissolved in anhydrous dichloromethane (37 mL) under argon. 1,1′-Carbonyldiimidazole (2 eq.) was added at room temperature. The reaction mixture was stirred for 40 min. The mixture was diluted with DCM, washed with water, dried over Na2SO4, and concentrated under vacuum. Compound 128 (19.39 g) was recovered as a pale yellow foam in 99% yield over two steps and in 98% purity (HPLC).

Provenance & Evidence