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The synthesis of tritium, carbon‐14 and stable isotope labelled selective estrogen receptor degraders
Author(s) -
Bragg Ryan A.,
Bushby Nick,
Ericsson Cecilia,
Kingston Lee P.,
Ji Hailong,
Elmore Charles S.
Publication year - 2016
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3437
Subject(s) - chemistry , tritium , stable isotope ratio , carbon 14 , radiochemistry , bioavailability , estrogen receptor , isotopes of carbon , chemical synthesis , estrogen , isotope , carbon fibers , combinatorial chemistry , environmental chemistry , stereochemistry , organic chemistry , biochemistry , pharmacology , total organic carbon , medicine , in vitro , breast cancer , cancer , physics , quantum mechanics , nuclear physics , materials science , composite material , composite number
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‐1 H ‐pyrido[3,4‐b]indol‐1‐yl)phenyl]prop‐2‐enoic acids were required. This paper discusses 5 synthetic approaches to this compound class.
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