Highly diastereoselective synthesis of benzothiazolo[3,2-a]pyridines via [4 + 2] annulation reaction of 2-vinylbenzothiazoles and azlactones

]pyridine derivatives was readily obtained in good to excellent yields (68-96%), with high diastereoselectivities and tolerating quite a broad scope of substituents. By using chiral phosphoric acid catalyst, the desired products were obtained in high enantioselectivities, up to -94%. This methodology provides a rapid and useful method for constructing fused benzothiazole derivatives.