Gram-Scale Laboratory Synthesis of TC AC 28, a High-Affinity BET Bromodomain Ligand

Raysa Khan, Graham Marsh, Robert Felix, Paul D. Kemmitt, Matthias G. J. Baud, Alessio Ciulli, John Spencer (Lead / Corresponding author)

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Abstract

TC AC 28, 6-(1H-Indol-4-yl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetic acid methyl ester, has been synthesized on a near-gram scale in seven steps with notable improvements in the reported poor-yielding last two steps enabling this key chemical probe compound to be available for researchers.

Original languageEnglish
Pages (from-to)4328-4332
Number of pages5
JournalACS Omega
Volume2
Issue number8
Early online date8 Aug 2017
DOIs
Publication statusPublished - Aug 2017

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    Khan, R., Marsh, G., Felix, R., Kemmitt, P. D., Baud, M. G. J., Ciulli, A., & Spencer, J. (2017). Gram-Scale Laboratory Synthesis of TC AC 28, a High-Affinity BET Bromodomain Ligand. ACS Omega, 2(8), 4328-4332. https://doi.org/10.1021/acsomega.7b00780