Maxim A. Novikov , Konstantin V. Potapov , Roman A. Novikov , Pavel N. Solyev , Yury V. Tomilov , Sergey N. Kochetkov , Alexander A. Makarov , Vladimir A. Mitkevich
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引用次数: 0
Abstract
A convenient and efficient synthesis of 3-{[6-(7-chloro- benzo[b]thiophen-2-yl)-1H-indol-1-yl]methyl}-1H-pyrazole- 5-carboxylic acid (NL3), which is currently among the most active and promising bacterial cystathionine γ-lyase (bCSE) inhibitors, has been developed. It is based on shifting the key stage of [Pd]-catalyzed cross-coupling of the indole and benzothiophene counterparts to the beginning of the synthetic scheme, with the polarity reversal of the components being coupled, to give 6-(7-chlorobenzo[b]thiophen-2-yl)-1H- indole as the key intermediate. The STD NMR method was used to estimate the NL3 compound obtained in the optimized synthesis as a ligand to saCSE (the main producer of H2S in pathogenic S. aureus).
期刊介绍：
Mendeleev Communications is the journal of the Russian Academy of Sciences, launched jointly by the Academy of Sciences of the USSR and the Royal Society of Chemistry (United Kingdom) in 1991. Starting from 1st January 2007, Elsevier is the new publishing partner of Mendeleev Communications.
Mendeleev Communications publishes short communications in chemistry. The journal primarily features papers from the Russian Federation and the other states of the former USSR. However, it also includes papers by authors from other parts of the world. Mendeleev Communications is not a translated journal, but instead is published directly in English. The International Editorial Board is composed of eminent scientists who provide advice on refereeing policy.
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