title: The synthesis of tritium, carbon-14 and stable isotope labelled selective estrogen receptor degraders.
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.
authors: Drug Safety & Metabolism, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Cambridgeshire, UK. ryan.bragg@astrazeneca.com.
authors: Ryan A
authors: RA
authors: Bragg
authors: Drug Safety & Metabolism, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Cheshire, UK.
authors: Nick
authors: N
authors: Bushby
authors: Drug Safety & Metabolism, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Mölndal, Sweden.
authors: Cecilia
authors: C
authors: Ericsson
authors: Drug Safety & Metabolism, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Mölndal, Sweden.
authors: Lee P
authors: LP
authors: Kingston
authors: Pharmaron Beijing, Co. Ltd, Beijing, China.
authors: Hailong
authors: H
authors: Ji
authors: Drug Safety & Metabolism, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Mölndal, Sweden.
authors: Charles S
authors: CS
authors: Elmore
mesh_terms: D001682:Biological Availability; D002250:Carbon Radioisotopes / Q000737:chemistry*; D060326:Chemistry Techniques, Synthetic; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D007553:Isotope Labeling; D011960:Receptors, Estrogen / Q000378:metabolism*; D014316:Tritium / Q000737:chemistry*
chemical_list: D002250:Carbon Radioisotopes; D007211:Indoles; D011960:Receptors, Estrogen; D014316:Tritium
keywords: carbon-14; cyanation; estrogen receptor degrader; tritium