Gram scale laboratory synthesis of TC AC 28, a high affinity BET bromodomain ligand.
Gram scale laboratory synthesis of TC AC 28, a high affinity BET bromodomain ligand.
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.
process control, Suzuki coupling reaction
4328-4332
Khan, Raysa
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Marsh, Graham
4c29af58-1128-444d-96cb-463e19642df2
Felix, Robert
acfd9272-cc4b-4838-bca1-8c31965d5a2e
Kemmitt, Paul D.
0f178e56-e8e2-4d3d-b8af-71d0f5641f19
Baud, Matthias G.J.
8752d519-3d33-43b6-9a77-ab731d410c2e
Ciulli, Alessio
6a734270-055b-47ed-b97d-51cff3fb50f1
Spencer, John
a3cf55cd-a4c7-4af6-b16c-96c8fb8c4cf4
31 August 2017
Khan, Raysa
ac317732-8e4c-4571-88b3-3b3f2372cec7
Marsh, Graham
4c29af58-1128-444d-96cb-463e19642df2
Felix, Robert
acfd9272-cc4b-4838-bca1-8c31965d5a2e
Kemmitt, Paul D.
0f178e56-e8e2-4d3d-b8af-71d0f5641f19
Baud, Matthias G.J.
8752d519-3d33-43b6-9a77-ab731d410c2e
Ciulli, Alessio
6a734270-055b-47ed-b97d-51cff3fb50f1
Spencer, John
a3cf55cd-a4c7-4af6-b16c-96c8fb8c4cf4
Khan, Raysa, Marsh, Graham, Felix, Robert, Kemmitt, Paul D., Baud, Matthias G.J., Ciulli, Alessio and Spencer, John
(2017)
Gram scale laboratory synthesis of TC AC 28, a high affinity BET bromodomain ligand.
ACS Omega, 2 (8), .
(doi:10.1021/acsomega.7b00780).
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.
Text
acsomega.7b00780
- Version of Record
Text
Tocris scale up paper 26517
More information
Accepted/In Press date: 25 July 2017
e-pub ahead of print date: 8 August 2017
Published date: 31 August 2017
Keywords:
process control, Suzuki coupling reaction
Identifiers
Local EPrints ID: 414041
URI: http://eprints.soton.ac.uk/id/eprint/414041
ISSN: 2470-1343
PURE UUID: 305bd465-8247-494a-93b5-1635c385e27c
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Date deposited: 13 Sep 2017 16:31
Last modified: 16 Mar 2024 05:43
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Contributors
Author:
Raysa Khan
Author:
Graham Marsh
Author:
Robert Felix
Author:
Paul D. Kemmitt
Author:
Alessio Ciulli
Author:
John Spencer
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