Efficient synthesis of a novel euchromatic histone methyl transferase 2 (G9a) inhibitor
Results in Chemistry(2022)
摘要
An efficient synthetic route was set up to prepare in good scale M-108, a novel bicycle derivative recently identified as a potent and selective G9a inhibitor, potentially useful as anti-fibroadipogenic agent. In particular, a facile three-steps sequential transformation of a substituted cis-cinnamate ethyl ester intermediate allowed to obtain the corresponding cyclopropyl nitrile derivative in high yield, which was smoothly transformed into the title racemate and then resolved by chiral HPLC.
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关键词
G9a inhibitor,Duchenne muscle dystrophy,Cyclopropanation,Chiral resolution
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