Abstract：
1,2-Diamination of alkenes represents an attractive way to generate differentiated vicinal diamines, which are prevalent motifs in biologically active compounds and catalysts. However, existing methods are usually limited in scope and produce diamines where one or both nitrogens are protected, adding synthetic steps for deprotection and further N-functionalization to reach a desired target. Furthermore, the range of amino groups that can be introduced at the internal position is fairly limited. Here we describe a 1,2-diamination of styrenes that directly installs a free amino group at the terminal position and a wide variety of unprotected nitrogen nucleophiles (primary or secondary alkyl or aromatic amines, sulfoximines, N-heterocycles, and ammonia surrogate) at the internal position. Two complementary sets of conditions encompass electronically activated and deactivated styrenes with diverse substitution patterns and functional groups. Moreover, this strategy can be extended to the 1,2-aminothiolation of styrenes.
摘要：
烯烃的1,2-二胺化代表了一种有吸引力的方法来产生分化的邻二胺，它们是生物活性化合物和催化剂中普遍存在的基序。然而,现有的方法通常是有限的范围和产生二胺，其中一个或两个氮被保护，添加用于脱保护和进一步N-官能化的合成步骤以达到期望的目标。此外，可以在内部位置引入的氨基的范围相当有限。在这里，我们描述了苯乙烯的1,2-二胺化，该苯乙烯直接在末端位置安装自由氨基和各种未保护的氮亲核体（伯或仲烷基或芳胺，磺基肟,N-杂环,和氨替代品)在内部位置。两组互补的条件包括具有不同取代模式和官能团的电子活化和失活苯乙烯。此外，该策略可以扩展到苯乙烯的1,2-氨基硫醇化。
