HCID 86709856, compound → HCID 86709855, compound

Participants

Reaction Steps

In yet another embodiment, the process provided herein for preparing 4-amino-2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione, or an enantiomer or a mixture of enantiomers thereof; or a pharmaceutically acceptable salt, solvate, hydrate, or polymorph thereof; comprises the steps of (i) reducing 2-(2,6-dioxopiperidin-3-yl)-5-methoxy-4-nitroisoindoline-1,3-dione with hydrogen in the presence of (a) a catalyst, in one embodiment, Pd/C; in (b) a solvent, in one embodiment, DMF; to form 4-amino-2-(2,6-dioxopiperidin-3-yl)-5-methoxyisoindoline-1,3-dione; and (ii) reacting form 4-amino-2-(2,6-dioxopiperidin-3-yl)-5-methoxyisoindoline-1,3-dione with BBr3 to 4-amino-2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione.

Provenance & Evidence