Structure of Elacestrant
Elacestrant API is featured with a chiral center. Elacestrant structure is formed by reacting with amine and aldehyde groups.
The Overall Synthesis of Elacestrant API
There are two essential routes leading to the syntehsis of Elacestrant API. One is from the innovator Radius Pharmaceuticals (lower part of the Elacestrant ROS map) and from a generic-CDMO route.
The Elacestrant intermediate (6R)-6-(2-amino-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol, CAS No. 2477812-39-6 whose racemic form is CAS No. 722520-36-7. It is to be reacted with the achiral moeity CAS No. 2477812-42-1, and forms the N-1 Elacestrant intermediate, which requires further reduction of the ketone group.
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