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Gram scale laboratory synthesis of TC AC 28, a high affinity BET bromodomain ligand

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posted on 2023-06-09, 07:28 authored by Raysa Khan, Graham Marsh, Robert Felix, Paul D Kemmitt, Matthias G J Baud, Alessio Ciulli, John SpencerJohn Spencer
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 2 steps enabling this key chemical probe compound to be available for researchers.

Funding

A Precompetitive Modular Peptidomimetic Toolkit for Targeting PPIs iCASE; G1436; EPSRC-ENGINEERING & PHYSICAL SCIENCES RESEARCH COUNCIL; EP/M507568/1

History

Publication status

  • Published

File Version

  • Published version

Journal

ACS Omega

ISSN

2470-1343

Publisher

American Chemical Society

Issue

8

Volume

2

Page range

4328-4332

Department affiliated with

  • Chemistry Publications

Full text available

  • Yes

Peer reviewed?

  • Yes

Legacy Posted Date

2017-07-28

First Open Access (FOA) Date

2017-08-10

First Compliant Deposit (FCD) Date

2017-07-27

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