A simple metal-free method has been developed for the reductive N-alkylation of indoles employing aldehydes as the alkylating agent and inexpensive EtSiH as the reductant. A wide range of aromatic and aliphatic aldehydes are viable substrates along with a variety of substituted indoles. In addition, the method was applied to a one-pot sequential 1,3-alkylation of a substituted indole and successfully demonstrated on a 100 mmol scale.
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| http://dx.doi.org/10.1021/acs.orglett.1c00179 | DOI Listing |
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