02048nas a2200229   4500008004100000022001400041245010800055210006900163260000900232300001400241490000700255520125900262653002101521653001001542653002201552100002201574700002201596700002901618700002601647700002001673856012501693       2023                        eng d  a1463-926200aIron-catalyzed regioselective C-H alkylation of indoles: an additive-free approach in renewable solvent0 aIroncatalyzed regioselective CH alkylation of indoles an additiv  cNOV   a9733-97430 v253 a<p>Alkylated indoles are important motifs in various biologically active molecules and drug candidates. Herein, we report a mild and efficient iron-catalyzed protocol for synthesizing alkylated indoles via C-H bond alkylation of indoles with unactivated alkenes, demonstrating a high level of regioselectivity. The reaction occurs under additive-free, solvent-free (or trace green solvent, 2-MeTHF) and less energy-intensive conditions using a sustainable metal catalyst and provides easy access to privileged alkylated indoles with anti-Markovnikov selectivity. Alkylation is compatible with important functionalities, such as fluoro, chloro, trifluoromethyl, alkenyl, ether, thioether, silyl, and siloxane, including heteroaryl, pyridinyl, carbazolyl, and indolyl moieties (45 examples, up to 96% yield). The developed protocol is very simple, straightforward, and fully accords with the principles of green chemistry. A detailed mechanistic investigation manifests the facile indole's C-H activation at the Fe(0) center, reversible 1,2-insertion of the alkene into the Fe-H bond of a metallacycle, and a turnover-limiting reductive elimination. Alkylated indoles are important motifs in various biologically active molecules and drug candidates.</p>
10aAromatic Ketones10aGreen10aorganic synthesis1 aPradhan, Chandini1 aJagtap, Rahul, A.1 aSamal, Pragnya, Paramita1 aKrishnamurty, Sailaja1 aPunji, Benudhar  uhttps://library.ncl.res.in/content/iron-catalyzed-regioselective-c-h-alkylation-indoles-additive-free-approach-renewable