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This paper reports a versatile, good-yielding, solution-phase method that is a substituent diversity-directed synthesis of 1H-indoles (6-13, 17-20) and 1-hydroxyindoles (14, 15) starting from commercially available 1,5-difluoro-2,4-dinitrobenzene. The synthetic products possessed the maximum six diversity points.


Dong Mei Wang, Ming Na Sun, Gang Liu. Substituent diversity-directed synthesis of indole derivatives. Journal of combinatorial chemistry. 2009 Jul-Aug;11(4):556-75

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PMID: 19469481

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