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Baumann, Andreas N.; Reiners, Felix; Juli, Thomas; Didier, Dorian (2018): Chemodivergent and Stereoselective Access to Fused Isoxazoline Azetidines and Thietanes through 3 + 2-Cycloadditions. In: Organic Letters, Vol. 20, No. 21: pp. 6736-6740
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By combining efficient methodologies for the preparation of substituted azetines and thietes with a highly regio- and diastereoselective 3 + 2-cycloaddition, a straightforward pathway for the synthesis of fused isoxazoline azetidines and thietanes has been designed. With minimal steps and starting from commercial sources, a new library of elaborated architectures was synthesized opening up a new class of molecules with large potential in pharmacology. Finally, a retro 2 + 2-cycloaddition leading to substituted isoxazoles is described.