1260909-30-5Relevant academic research and scientific papers
Catalytic asymmetric synthesis of indole derivatives as novel α-glucosidase inhibitors in vitro
Islam, Mohammad Shahidul,Barakat, Assem,Al-Majid, Abdullah Mohammed,Ali,Yousuf, Sammer,Iqbal Choudhary,Khalil, Ruqaiya,Ul-Haq, Zaheer
supporting information, p. 350 - 354 (2018/06/01)
Indole containing compounds have acquired conspicuous significance due to their wide spectrum of biological activities. Synthesis of a series of enantiomerically pure indole derivatives 3a-r via Friedel–Crafts alkylation of indole 1 with enones 2a-r were described here. The products were isolated in a moderate to excellent yields (upto 89%) with excellent enantioselectivities (upto 99.9% ee). These compounds 3a-r were evaluated for their in vitro α-glucosidase inhibitory activity and some of them were identified as potent inhibitors (IC50 = 4.3 ± 0.13–43.9 ± 0.51 μM) with several fold higher activity than the clinically used α-glucosidase inhibitor, acarbose (IC50 = 840 ± 1.73 μM). To the best of knowledge, this is the first report of the propanone substituted indole ring containing compounds by in vitro α-glucosidase enzyme inhibition.
Chiral Bronsted acid catalyzed asymmetric Friedel-Crafts alkylation reaction of indoles with α,β-unsaturated ketones: Short access to optically active 2- and 3-substituted indole derivatives
Sakamoto, Tsubasa,Itoh, Junji,Mori, Keiji,Akiyama, Takahiko
experimental part, p. 5448 - 5454 (2011/01/12)
The asymmetric Friedel-Crafts alkylation reaction of indoles with α,β-unsaturated ketones catalyzed by chiral phosphoric acid is reported. A wide range of indoles and 4,7-dihydroindoles were allowed to react with α,β-unsaturated ketones to give the corres
Highly enantioselective alkylation reaction of enamides by bronsted-acid catalysis
Guo, Qi-Xiang,Peng, Yun-Gul,Zhang, Jin-Wei,Song, Liu,Feng, Zhang,Gong, Liu-Zhu
supporting information; experimental part, p. 4620 - 4623 (2009/12/09)
The H8-BINOL-derived, phosphoric acid catalyzed, highly enatioselective alkylation reaction of enamides with Indoiyl alcohols has been described. A phosphoric acid derived from H8-BINOL enabled an asymmetric α-alkylation of enamides with indoiy
