Ultrasound Assisted One-pot and Sequential Synthesis of 3-methyleneisoindolin- 1-ones and their in vitro Evaluation

Abstract

The methodology involved coupling of (trimethylsilyl)acetylene with iodoarenes in the presence of 10% Pd/C-CuI-PPh3-Et3N in MeOH followed by treating the reaction mixture with K2CO3 in aqueous MeOH, and finally coupling with 2-iodo-N-(pyridin-2-ylmethyl)benzamide. The in vitro evaluation of these compounds was performed to identify some initial hit molecules one of which showed dose dependent inhibition of PDE4B.

Ultrasonic-assisted-synthesis of isoindolin-1-one derivatives

“…[14][15][16][17] Recent reports demonstrated that various substituted 3-methyleneisoindolin-1-ones and isoquinolin-1(2H)-ones have been generated in good yields in shorter reaction time via metal-catalyzed-cascade reaction (comprising of Sonogashira type coupling-heterocyclization reactions) under ultrasonic irradiation. [18][19][20] Due to these valuable features, the ultrasonic irradiation has been widely employed in organic synthesis and industrial process.…”

Inversion kinetics of some E/Z 3-(benzylidene)-2-oxo-indoline derivatives and their in silico CDK2 docking studies

“…It has been established for more than half a century that stereochemistry is fundamental in biological activities. 20,21 The stereoselection, which has been extensively studied, was almost exclusively explained in terms of diastereoselective interactions for sunitinib and related compounds. Interestingly, these molecules were bound as the Z-diastereomer, even though they were the E-diastereomer in solution.…”