Phthalimide → HCID 118214741, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of tert-butyl ((1S)-1-(6-(3-hydroxypiperidin-1-yl)-1-methyl-1H-pyrrolo[3,2-b]pyridin-5-yl)ethyl)carbamate (300 mg, 0.802 mmol), isoindoline-1,3-dione (165 mg, 1.12 mmol) and PPh3 (377 g, 1.44 mmol) in THF (2 mL) was stirred at 0° C. Next, diethyl azodicarboxylate (251 mg, 1.44 mmol) was added dropwise at 0° C., and the mixture was stirred at 20° C. for 16 hours. The solvent was evaporated in vacuo, and the residue was purified by preparative TLC to give the title compound as a white solid (100 mg, 35.2%). ESI-MS m/z [M+H]+ calc'd for C28H33N5O4, 504. found 504.

Provenance & Evidence