Work

Practical Synthesis of Elacestrant, an FDA‐Approved Selective Estrogen Receptor Degrader

Year: 2025

Type: article

Abstract: Herein, we report an efficient and scalable synthesis of the core skeleton of elacestrant, a selective estrogen receptor degrader used in breast cancer treatment. The present synthesis features simple synthetic transformations, involving one‐pot conversion of 6‐hydroxy‐1‐tetralone into a cyclic olefin followed by copper‐catalyzed arylation of the cyclic olefin (iodometathesis) with a diaryliodonium salt as a key strategy to achieve the core skeleton on a gram scale. This procedure was extended to the total synthesis of (±)‐elacestrant by employing two different coupling strategies: reductive amination of an aldehyde and nucleophilic substitution of a bromo compound with the core skeleton.

Source: European Journal of Organic Chemistry

DOI: 10.1002/ejoc.202501030

Authors: Chandra Shekhar, Pranay Kothuri, Srivari Chandrasekhar, Kiranmai Nayani

Institutions: Indian Institute of Chemical Technology, Academy of Scientific and Innovative Research

Language: English

Topic: Estrogen and related hormone effects

Subfield: Genetics

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: bronze

Funders: Council of Scientific and Industrial Research, India, University Grants Commission, Science and Engineering Research Board