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The synthesis of tritium, carbon-14 and stable isotope labelled selective estrogen receptor degraders
Ryan A Bragg1, Nick Bushby2, Cecilia Ericsson3
1Drug Safety & Metabolism, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Cambridgeshire, UK. ryan.bragg@astrazeneca.com.
Journal of Labelled Compounds & Radiopharmaceuticals
|August 26, 2016
Abstract:
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.

