A novel tandem method to synthesize 2-azaaryl indoline promoted by LiN(SiMe) from 2-azaaryl methyl amine and 2-fluoro benzyl bromides was developed. Mechanistic investigation indicated that this tandem cyclization was initiated by selective benzyl C-S2 substitution followed by an intramolecular SAr reaction. Diverse 2-azaaryl indoles could also be obtained simple functional transformations.
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| http://dx.doi.org/10.1039/d3ob01444d | DOI Listing |
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