Preprint Article Version 1 This version is not peer-reviewed

New Developments in the Synthesis of EMICORON

Version 1 : Received: 26 July 2018 / Approved: 26 July 2018 / Online: 26 July 2018 (14:25:19 CEST)

A peer-reviewed article of this Preprint also exists.

Pitorri, M.; Franceschin, M.; Serafini, I.; Ciccòla, A.; Frezza, C.; Bianco, A. New Developments in the Synthesis of EMICORON. High-Throughput 2018, 7, 22. Pitorri, M.; Franceschin, M.; Serafini, I.; Ciccòla, A.; Frezza, C.; Bianco, A. New Developments in the Synthesis of EMICORON. High-Throughput 2018, 7, 22.

Journal reference: High-Throughput 2018, 7, 22
DOI: 10.3390/ht7030022

Abstract

In this paper, the modification of two synthetic steps to obtain EMICORON, with respect to the usual protocol, is reported. EMICORON is a benzo[ghi]perylen-diimmide which was synthesized the first time in our laboratory in 2012 and showed to have in-vivo antitumor activities interfering with tumor growth and development by a multi-target mechanism of action. The provided modifications regarded the reaction times and the reaction conditions as well as the work-up procedures and allowed to increase the global yield of the process from 28% to about 40%. Thus, this new procedure may be more suitable in order to get larger amounts of EMICORON for further preclinical studies.

Subject Areas

EMICORON; organic synthesis; synthesis improvements; G-quadruplex structures; anticancer activity

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