Qin, Jingyang published the artcileCatalytic Atroposelective Electrophilic Amination of Indoles, Name: 2-(tert-Butyl)-5-chloro-1H-indole, the main research area is sulfonyl arylaminoindole preparation enantioselective chemoselective anticancer activity DFT; Amination; Atroposelectivity; Conjugation; C−N Axis; Heterocycles.
The first catalytic atroposelective electrophilic amination of indoles I (R = 2-t-Bu, 4-Me, 5-Ph), which delivers functionalized atropochiral N-sulfonyl-3-arylaminoindoles II (R1 = Boc, (4-methylphenyl)sulfonyl, (1-naphthyl)sulfonyl, etc.) with excellent optical purity was reported. This reaction was furnished by 1,6-nucleophilic addition to p-quinone diimines III. Control experiments suggest an ionic mechanism that differs from the radical addition pathway commonly proposed for 1,6-addition to quinone III (R1 = (4-methylphenyl)sulfonyl). The origin of 1,6-addition selectivity was investigated through computational studies. Preliminary studies show that the obtained 3-aminoindoles atropisomers II exhibit anticancer activities. This method was valuable with respect to enlarging the toolbox for atropochiral amine derivatives II.
Angewandte Chemie, International Edition published new progress about Amination catalysts (chemo-, stereoselective). 69622-40-8 belongs to class indole-building-block, name is 2-(tert-Butyl)-5-chloro-1H-indole, and the molecular formula is C12H14ClN, Name: 2-(tert-Butyl)-5-chloro-1H-indole.
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Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles