24486-66-6Relevant articles and documents
Intramolecular Addition of a Dimethylamino C(sp 3)-H Bond across C-C Triple Bonds Using IrCl(DTBM-SEGPHOS)(ethylene) Catalyst: Synthesis of Indoles from 2-Alkynyl- N -methylanilines
Ohmura, Toshimichi,Yagi, Kaito,Torigoe, Takeru,Suginome, Michinori
, p. 3057 - 3064 (2021/06/28)
Intramolecular addition of a C(sp 3)-H bond of the dimethylamino group across the C-C triple bond in 2-alkynyl- N, N -dimethylanilines is effectively catalyzed by a new iridium complex, IrCl(DTBM-SEGPHOS)(C 2H 4), in mesitylene at 150 °C. The intramolecular C(sp 3)-H addition is followed by double-bond isomerization to afford 3-substituted indoles in good to high yields.
Indole-based allosteric inhibitors of HIV-1 integrase
Patel, Pratiq A.,Kvaratskhelia, Nina,Mansour, Yara,Antwi, Janet,Feng, Lei,Koneru, Pratibha,Kobe, Mathew J.,Jena, Nivedita,Shi, Guqin,Mohamed, Mosaad S.,Li, Chenglong,Kessl, Jacques J.,Fuchs, James R.
supporting information, p. 4748 - 4752 (2016/09/13)
Employing a scaffold hopping approach, a series of allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) have been synthesized based on an indole scaffold. These compounds incorporate the key elements utilized in quinoline-based ALLINIs for binding to the IN dimer interface at the principal LEDGF/p75 binding pocket. The most potent of these compounds displayed good activity in the LEDGF/p75 dependent integration assay (IC50?=?4.5?μM) and, as predicted based on the geometry of the five- versus six-membered ring, retained activity against the A128T IN mutant that confers resistance to many quinoline-based ALLINIs.
A highly efficient route to C-3 alkyl-substituted indoles via a metal-free transfer hydrogenation
Chen, Cai,Feng, Huan-Xi,Li, Zhi-Long,Cai, Pin-Wen,Liu, Yan-Kai,Shan, Lian-Hai,Zhou, Xian-Li
, p. 3774 - 3776 (2014/07/07)
A highly efficient route to C-3 alkyl-substituted indoles via completely metal-free catalytic transfer hydrogenation of 3-indolemethanols was developed. This process proceeds via vinylogous iminium intermediates formed in situ in the presence of Br?nsted