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Synthesis of Hydroxylactams and Esters Derived from Thalidomide and Their Antitumor Activities

G Sun, X Liu, H Zhou, Z Liu, Z Mao

文献索引:Sun, Guanglong; Liu, Xiangchao; Zhou, Heng; Liu, Zenglu; Mao, Zhenmin Bulletin of the Korean Chemical Society, 2014 , vol. 35, # 5 p. 1337 - 1342

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摘要

A novel and convenient route for the synthesis of a series of thalidomide derivatives is described. Compound 2 was cyclized with different amines under alkaline condition to obtain 4-nitro substituted phthalimidines 3a-d. Hydroxylactams 4a-d were produced via bromination and hydroxylation. Different acyl chlorides were reacted with hydroxylactams to provide the desired esters 5a-d. All compounds were evaluated by MTT assay for their ...