Pyrrolidine → HCID 57762788, compound

Participants

Reaction Steps

Diphenylphosphoryl azide (290 μL; 1.36 mmol) was added in one portion to a stirring mixture of 4-[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]benzoic acid (195 mg; 0.63 mmol) and diisopropylethylamine (220 μL; 1.29 mmol) in 1,4-dioxane (2.2 mL). The mixture was heated at reflux for 2 hours, pyrrolidine (100 μL; 1.21 mmol) was added in on portion, and the reaction heated at reflux for a further 1 hour. Concentration in vacuo, followed by column chromatography gave the title compound (38 mg; 16%).

Provenance & Evidence