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高亲和力BET溴结构域配体TC AC 28的克级实验室合成

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

作者信息

Khan Raysa, Marsh Graham, Felix Robert, Kemmitt Paul D, Baud Matthias G J, Ciulli Alessio, Spencer John

机构信息

Department of Chemistry, School of Life Sciences, University of Sussex, Falmer, Brighton BN1 9QJ, U.K.

Tocris Bioscience, the Watkins Building, Atlantic Road, Avonmouth, Bristol BS11 9QD, U.K.

出版信息

ACS Omega. 2017 Aug 8;2(8):4328-4332. doi: 10.1021/acsomega.7b00780. eCollection 2017 Aug 31.

DOI:10.1021/acsomega.7b00780
PMID:31457724
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6641879/
Abstract

, 6-(1-Indol-4-yl)-8-methoxy-1-methyl-4-[1,2,4]triazolo[4,3-][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.

摘要

6-(1-吲哚-4-基)-8-甲氧基-1-甲基-4-[1,2,4]三唑并[4,3-][1,4]苯二氮䓬-4-乙酸甲酯已通过七步反应以近克级规模合成，在报道的产率较低的最后两步中取得了显著改进，使这种关键的化学探针化合物可供研究人员使用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf50/6641879/2cf109cf511f/ao-2017-00780a_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf50/6641879/6106cbc60346/ao-2017-00780a_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf50/6641879/2cf109cf511f/ao-2017-00780a_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf50/6641879/6106cbc60346/ao-2017-00780a_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf50/6641879/2cf109cf511f/ao-2017-00780a_0003.jpg

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