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)

Research output: Contribution to journalArticle

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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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Acetic acid
Esters
Ligands
methyl acetate
Bz-423

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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
Khan, Raysa ; Marsh, Graham ; Felix, Robert ; Kemmitt, Paul D. ; Baud, Matthias G. J. ; Ciulli, Alessio ; Spencer, John. / Gram-Scale Laboratory Synthesis of TC AC 28, a High-Affinity BET Bromodomain Ligand. In: ACS Omega. 2017 ; Vol. 2, No. 8. pp. 4328-4332.
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Khan, R, Marsh, G, Felix, R, Kemmitt, PD, Baud, MGJ, Ciulli, A & Spencer, J 2017, 'Gram-Scale Laboratory Synthesis of TC AC 28, a High-Affinity BET Bromodomain Ligand', ACS Omega, vol. 2, no. 8, pp. 4328-4332. https://doi.org/10.1021/acsomega.7b00780

Gram-Scale Laboratory Synthesis of TC AC 28, a High-Affinity BET Bromodomain Ligand. / Khan, Raysa; Marsh, Graham; Felix, Robert; Kemmitt, Paul D.; Baud, Matthias G. J.; Ciulli, Alessio; Spencer, John (Lead / Corresponding author).

In: ACS Omega, Vol. 2, No. 8, 08.2017, p. 4328-4332.

Research output: Contribution to journalArticle

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