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Tetrahydrophthalazine derivatives have found important applications in pharmaceutical research, but existing synthetic methods are unable to access them regio‐ and stereoselectively. Here, a new approach is presented that addresses these challenges by utilizing a 6‐endo‐trig radical cyclization in the key step. The desired tetrahydrophthalazines can be accessed in high yields (55–98 %) and high diastereoselectivities...
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