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.
Efficient synthesis of a novel euchromatic histone methyl transferase 2 (G9a) inhibitor / Gornati, D.; Sinisi, R.; Bertuolo, S.; De Matteo, M.; Di Fabio, R.. - In: RESULTS IN CHEMISTRY. - ISSN 2211-7156. - 4:(2022). [10.1016/j.rechem.2022.100654]
Efficient synthesis of a novel euchromatic histone methyl transferase 2 (G9a) inhibitor
Di Fabio R.
2022-01-01
Abstract
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
