Maolin Sun, Jianchang Li, Chaoming Liang
Nov 9, 2020
Citations
0
Influential Citations
4
Citations
Journal
Journal of Flow Chemistry
Abstract
2-Pyridyl ketones widely appear in bioactive molecules, natural products, and are employed as precursors of chiral 2-pyridine alky/aryl alcohols or 2-aminoalkyl pyridine ligands for asymmetric catalysis. Herein, a practical method for the rapid synthesis of 2-pyridyl ketone library in continuous flow is reported, in which the 2-lithiopyridine formed by Br/Li exchange reacts with commercially available esters to obtain 2-pyridyl ketones in a good yield at short reaction time. This protocol functions broadly on a variety of esters and has been applied to the synthesis of TGF-β type 1 receptor inhibitor LY580276 intermediate in an environmentally friendly method. It is rapid, reliable, and cost-efficient to afford diverse kinds of 2-pyridyl ketones in the compound library. Graphical abstract A practical method for therapid synthesis of 2-pyridyl ketones under continuous flow using simple estersand 2-bromopyridine was reported. This procedure iswidely applicable to aromatic esters, alkyl esters, N-Boc amino acidmethyl esters, α-bromoesters and dimethyl oxalate, leading to variousfunctionalized 2-pyridyl ketones with good yields A practical method for therapid synthesis of 2-pyridyl ketones under continuous flow using simple estersand 2-bromopyridine was reported. This procedure iswidely applicable to aromatic esters, alkyl esters, N-Boc amino acidmethyl esters, α-bromoesters and dimethyl oxalate, leading to variousfunctionalized 2-pyridyl ketones with good yields