PROCESS FOR PREPARATION OF 4-AMINO-2-(2,6-DIOXOPIPERIDIN-3-YL)ISOINDOLINE-1,3-DIONE COMPOUND

摘要

PROBLEM TO BE SOLVED: To provide a new process for the preparation of unsubstituted or substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds which are a therapeutic agent for diseases related to an abnormally high level or activity of TNF-α.

SOLUTION: The process includes a step of cyclizing a compound of formula (II) or (IIA) or a salt thereof with a cyclizing agent of formula (V). In the formulas, R1is H, F, benzyl, (C1-C8) alkyl, (C2-C8) alkenyl or (C2-C8) alkynyl, and X and Y are each independently unsubstituted or substituted imidazolyl, benzimidazolyl, or benzotriazolyl.

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