Methods for synthesizing 3-(substituted dihydroisoindolinone-2-yl)-2, 6-dioxopiperidine, and intermediates thereof

摘要

The present invention discloses methods for synthesizing 3-(substituted dihydroisoindolinone-2-yl)-2,6-dioxopiperidine and intermediates thereof, namely, the synthesis of compounds of the Formula (I), with each substitutional group defined in the patent specification. Owing to the advantages of high productivity, little influence to the environment and material accessibility, the methods of the present invention is suitable for industrial production.;

主权项

1. A method for synthesizing the compound of Formula (I), comprising:reacting a compound of Formula (II) with a compound of Formula (III) to yield a compound of Formula (IV);wherein:
One of R, R3, R4 and R5 is amino or protected amino, nitro or halo, and the others are all hydrogen; X is halo; Y is: ═O or H; Z is: ═O or H; and with proviso that Y and Z are both ═O; or one of Y and Z is ═O, and the other is H; R′ is alkali metal ion or hydrogen or imine protecting group; A and B are each independently hydroxyl, C1-10 alkoxy, aryloxy, aryl C1-4 alkoxy or NHR2, and wherein, R2 is hydrogen or amino protecting group; R1 is C1-4 alkyl or hydrogen.