3-Aminopiperidine-2,6-dione hydrochloride → 2-(2,6-Dioxopiperidin-3-yl)-5-nitro-1H-isoindole-1,3(2H)-dione

Participants

Reaction Steps

The same patents also describe the preparation of the nitro intermediate. 4-Nitro-phthalic anhydride is coupled with 2,6-dioxopiperidine-3-ammonium chloride in glacial acetic acid and sodium acetate to obtain 1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)-5-nitro-isoindoline in 54% yield. The preparation of the nitro intermediate 3-(1-oxo-4-nitro-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione follows the same reaction conditions as described, resulting in a low yield of the nitro intermediate of about 55%.

Provenance & Evidence