A new facile, efficient and very mild entry to the synthesis of 3-（1H-indol-3-yl）-1, 3-diarylpropan-l-ones is presented. The procedure utilizes phosphotungstic acid （5 mol%） as a catalyst for the Michael addition ...A new facile, efficient and very mild entry to the synthesis of 3-（1H-indol-3-yl）-1, 3-diarylpropan-l-ones is presented. The procedure utilizes phosphotungstic acid （5 mol%） as a catalyst for the Michael addition of indole to α,β-unsaturated ketones in good yield in acetonitrile as solvent.展开更多
Highly enantioselective sulfa-Michael additions(SMA)between 2-alkenyl quinoxalines and aromatic thiols are accomplished using a low loading of chiral phosphoric acid catalyst(1 mol%).It was confirmed by an investigati...Highly enantioselective sulfa-Michael additions(SMA)between 2-alkenyl quinoxalines and aromatic thiols are accomplished using a low loading of chiral phosphoric acid catalyst(1 mol%).It was confirmed by an investigation of a lot of azaarenes that the two C-N units of quinoxalines are indispensable for controlling the reaction enantioselectivities.A series of non-terminal 2-alkenes substituted with aryls or alkyls,even other electro-withdrawing groups such as ketones,esters,or amides,selectively reacted and afforded the desired SMA products(48 examples)in good regioselectivities with high yields(up to 99%)and good ee values(up to 97%).展开更多
文摘A new facile, efficient and very mild entry to the synthesis of 3-（1H-indol-3-yl）-1, 3-diarylpropan-l-ones is presented. The procedure utilizes phosphotungstic acid （5 mol%） as a catalyst for the Michael addition of indole to α,β-unsaturated ketones in good yield in acetonitrile as solvent.
基金supported by the West Light Foundation of the Chinese Academy of Sciences(No.25E0C304)the Sichuan Science and Technology Program(No.2021ZYD0061).
文摘Highly enantioselective sulfa-Michael additions(SMA)between 2-alkenyl quinoxalines and aromatic thiols are accomplished using a low loading of chiral phosphoric acid catalyst(1 mol%).It was confirmed by an investigation of a lot of azaarenes that the two C-N units of quinoxalines are indispensable for controlling the reaction enantioselectivities.A series of non-terminal 2-alkenes substituted with aryls or alkyls,even other electro-withdrawing groups such as ketones,esters,or amides,selectively reacted and afforded the desired SMA products(48 examples)in good regioselectivities with high yields(up to 99%)and good ee values(up to 97%).
