Efficient synthesis of a novel euchromatic histone methyl transferase 2 (G9a) inhibitor

Autor: Davide Gornati, Roberta Sinisi, Stefania Bertuolo, Marilenia De Matteo, Romano Di Fabio
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: Results in Chemistry, Vol 4, Iss , Pp 100654- (2022)
Druh dokumentu: article
ISSN: 2211-7156
DOI: 10.1016/j.rechem.2022.100654
Popis: 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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