The synthesis of tritium, carbon-14 and stable isotope labelled selective estrogen receptor degraders

As part of a Medicinal Chemistry program aimed at developing an orally bioavailable selective estrogen receptor degrader, a number of tritium, carbon‐14, and stable isotope labelled (E)‐3‐[4‐(2,3,4,9‐tetrahydro‐1H‐pyrido[3,4‐b]indol‐1‐yl)phenyl]prop‐2‐enoic acids were required. This paper discusses 5 synthetic approaches to this compound class. As part of a Medicinal Chemistry program aimed at developing an orally bioavailable selective estrogen receptor degrader, a number of tritium, carbon‐14, and stable isotope labelled (E)‐3‐[4‐(2,3,4,9‐tetrahydro‐1H‐pyrido[3,4‐b]indol‐1‐yl)phenyl]prop‐2‐enoic acids were required. This paper discusses 5 synthetic approaches to this compound class.