Phthalimide → HCID 69248953, compound

Participants

Reaction Steps

To a solution of compound (ii) (5 mg, 0.009 mmol), triphenylphosphine (3.6 mg, 0.014 mmol) and phthalimide (2.0 mg, 0.014 mmol) in THF (0.5 mL) was added diisopropyl azodicarboxylate (2.7 μL, 0.014 mmol) at 0° C. After the mixture had been stirred at RT for 3.5 h, more triphenylphosphine (3.6 mg, 0.014 mmol), phthalimide (2.0 mg, 0.014 mmol) and DIAD (2.7 μL, 0.014 mmol) were added and stirring was continued at RT for a further 40 min. The solvent was removed in vacuo and the residue was purified by preparative LCMS (5-50-100% ACN in 0.1% aqueous formic acid) to afford 5-cyclopropyl-6-[3-(1,3-dioxoisoindolin-2-yl)propyl-methylsulfonyl-amino]-2-[4-(4-fluoroanilino)phenyl]-N-methyl-indazole-3-carboxamide (iii) as a white solid (20 mg, 81%).

Provenance & Evidence