Straightforward protocol for the efficient synthesis of varied N-acylated (aza)indole 2-/3-alkanoic acids and esters: optimization and scale-up |
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| Authors: | Andy J LiedtkeKwangho Kim Donald F StecGary A Sulikowski Lawrence J Marnett |
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| Institution: | a A.B. Hancock Jr. Memorial Laboratory for Cancer Research, Departments of Biochemistry, Chemistry and Pharmacology, Vanderbilt Institute of Chemical Biology, Center in Molecular Toxicology and Vanderbilt-Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
b Departments of Chemistry and Biochemistry, Vanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, TN 37235, USA |
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| Abstract: | A library of approximately 40 N1-acylated (aza)indole alkanoic esters and acids was prepared employing a microwave-assisted approach. The optimized synthetic route allows for parallel synthesis, variation of the indole substitution pattern, and high overall yield. Additionally, the procedure has been scaled up to yield multi-gram amounts of preferred indole compounds, e.g.: 2′-des-methyl indomethacin 2. The reported compounds were designed as biomedical tools for primary and secondary in vitro and in vivo studies at relevant molecular targets. |
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| Keywords: | Heterocyles Indoles (2&prime -Des-methyl) indomethacin Microwave synthesis Synthesis scale-up |
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