A Scalable, Chromatography-Free Synthesis of the Potent and Highly Selective ERβ Agonist EGX358

Abstract

4-[trans-4-(Hydroxymethyl)cyclohexyl]phenol (EGX358) is a potent and highly selective estrogen receptor beta (ERβ) agonist which has demonstrated efficacy for moderation of a chemically induced hot flash and for memory consolidation in an ovariectomized mouse model for menopause. An improved synthetic route to EGX358 is reported which proceeds in four steps and which is chromatography-free.

Key words

chromatography-free synthesis - Diels–Alder reaction - ionic reduction - estrogen receptor beta agonist - EGX358

Publication History

Received: 11 November 2024

Accepted after revision: 11 December 2024

Article published online:
22 January 2025

• References

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