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New method for synthesis of EZH2 methyltransferase inhibitor GSK126

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Version 2 2016-07-13, 18:10
Version 1 2016-06-02, 19:19
journal contribution
posted on 2016-07-13, 18:10 authored by Chen Lu, Qiang Zhang, Xin Chen

GSK126 is a potent small-molecule inhibitor of S-adenosyl-methionine-competitive EZH2 methyltransferase and has the potential to be used clinically for preventing unwanted histone methylation of tumor suppressor genes. In this article, we describe a new synthetic route that has been developed for synthesizing the title compound through nine steps, starting from 2,5-dibromobenzoic acid. This synthetic method is economical and suitable for multigram-scale preparation of GSK126 and related N-alkylated indole derivatives.

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