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Synthesis of isoindolines

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A facile method provides N-aryl-substituted azacycles from arylamines and cyclic ethers in the presence of POCl3 and DBU. Using this method, various azacycloalkanes, isoindolines, and tetrahydroisoquinolines were prepared in high yields. This synthetic method offers an efficient approach to the production of five- and six-membered azacycles.
M. T. La, S. Kang, H.-K. Kim, J. Org. Chem., 2019, 84, 6689-6696.


Acid-catalysed intramolecular hydroamination of 2-alkenylarylethylamine derivatives gives smoothly isoindolines via benzylic carbenium ion generation.
L. Henderson, D. W. Knight, A. C. Williams, Synlett, 2012, 23, 1667-1669.


Synergistic palladium and Brønsted acid catalysis enables a diastereoselective cyclization of chiral sulfinamides as nucleophiles to provide chiral isoindolines with good yields and high diastereoselectivities.
C.-T. Hung, C.-W. Lu, S.-H. Huang, Y.-F. Lu, H.-C. Chou, C.-C. Tsai, J. Org. Chem., 2021, 86, 12354-12366.