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.
Authors
- Subhabrata Chaudhury (ORCID: https://orcid.org/0000-0002-2022-2677)
- Dulanjali Thennakoon
- Edward A. Wetzel (ORCID: https://orcid.org/0000-0002-8058-6819)
- William A. Donaldson (ORCID: https://orcid.org/0000-0002-0840-3731)
Institutions
- Marquette University (US)
- NewGen Therapeutics (United States) (US)
Publication Details
- Journal
- Synthesis
- Published
- 2025-01-22
- DOI
- https://doi.org/10.1055/s-0043-1775433
- Primary Topic
- Protein Kinase Regulation and GTPase Signaling
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- National Institute on Aging
- National Institute of General Medical Sciences