950190-45-1

Upstream product

• 120-72-9 indole 
• 959-33-1 3-(4-methoxyphenyl)-1-phenylprop-2-en-1-one 
• 30925-52-1 (2Z)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-one 

Relevant academic research and scientific papers

Catalytic asymmetric synthesis of indole derivatives as novel α-glucosidase inhibitors in vitro

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.

ALPHA-GLUCOSIDASE INHIBITORS

Novel α-Glucosidase inhibitors include propanone substituted indole ring-containing heterocyclic compounds, which are represented by Formula I: Wherein R1 is thiophene, 2,4-di chloro phenyl, 2,6-di chloro phenyl, bromo phenyl, benzyl or nitrophenyl; and R2 is an aryl group, or stereoisomers or pharmaceutically acceptable salts thereof.

Highly enantioselective Friedel-Crafts alkylation of indoles with α,β-unsaturated ketones with simple Cu(II)-oxazoline-imidazoline catalysts

A series of novel chiral ligands L1-L4 with an imidazoline-oxazoline framework have been developed as new type of non-symmetric N,N-bidentate ligands. All the chiral ligands were prepared from 2,2-diethylmalonic acid and enantiomerically pure (S)-2-amino-