Synthesis of WAY-163909; a selective 5-HT2CR agonist

A new synthetic approach to derivatives the serotonin 2C receptor (5-HT2CR) agonist WAY-163909 is reported. In addition to the WAY-163909 versions possessing a site that has been shown to accommodate the attachment of linkers without loss of agonist activity are accessible by this approach. An efficient 7 step synthesis with an overall 32% yield is reported. (C) 2022 Elsevier Ltd. All rights reserved.

Automated summary

A new synthetic approach for the serotonin 2C receptor agonist WAY-163909 is reported in this article. The approach allows the creation of WAY-163909 versions that possess a site for linker attachment without loss of agonist activity. An efficient 7-step synthesis with a 32% overall yield is described.