Synthesis and anticholinesterase activity of 2-substituted-N-alkynylindoles?
Organic & Biomolecular Chemistry Pub Date: 2018-10-04 DOI: 10.1039/C8OB02165A
Abstract
In this paper, we report a protocol for the preparation of 2-substituted-N-alkynylindoles via metalation of N-alkynylindoles followed by the capture of a 2-indolyl lithium intermediate with different electrophiles. The reactivity of the indoles prepared was also demonstrated through the reaction with CBr4/Ph3P for the preparation of 2-gem-dibromovinyl N-alkynylindoles and the hydrotelluration reaction of N-alkynylindoles, which led to vinylic tellurides. Some compounds prepared showed AChE inhibitory potential in the low micromolar range similar to that obtained with donepezil, a commercially available cholinesterase inhibitor.
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Journal Name：Organic & Biomolecular Chemistry
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CAS no.: 89640-58-4
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