SCHEDULED MAINTENANCE
Palladium-catalysed stereoselective [3 + 2] annulation of vinylethylene carbonates and tryptanthrin-based ketones†
Jun-Long
Li, 
*b
*b
Abstract
The palladium-catalysed [3 + 2] annulation of vinylethylene carbonates (VECs) and ketones remains challenging in organic synthesis. Herein, we successfully achieved the [3 + 2] annulation of tryptanthrin-based ketones and VECs for the efficient synthesis of indoloquinazolinone derivatives with generally excellent yields and good diastereoselectivity. Notably, the asymmetric version of this [3 + 2] annulation can also be achieved by using a chiral spiroketal-based diphosphine ligand. In addition, preliminary biological studies reveal that some of the products exhibit promising antibacterial activity.
![Graphical abstract: Palladium-catalysed stereoselective [3 + 2] annulation of vinylethylene carbonates and tryptanthrin-based ketones](/en/Image/Get?imageInfo.ImageType=GA&imageInfo.ImageIdentifier.ManuscriptID=D1QO01543E&imageInfo.ImageIdentifier.Year=2022)
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