作者:Scarpa de Souza, Edson Leonardo、Gorbatov, Sergei Aleksandrovich、Pierozzi, Breno Mendes、Batista Junior, João Marcos、Duarte Correia, Carlos Roque
DOI:10.1002/chem.202401115
日期:——
A one-pot tandem protocol is reported for the enantioselective Pd-catalyzed synthesis of dihydrobenzofuran, dihydroindole, and dihydrobenzosulfone scaffolds by a Heck-Matsuda reaction under open-flask conditions with in situ generation of aryldiazonium salt directly from anilines. The enantioenriched heterocycles are synthesized in overall yields up to 78 % in enantiomeric ratios up to 99 : 1 by a
报道了一种一锅串联方案,用于在开瓶条件下通过 Heck-Matsuda 反应对映选择性 Pd 催化合成二氢苯并呋喃、二氢吲哚和二氢苯砜支架,并直接从苯胺原位生成芳基重氮盐。通过顺序 5 步方案合成的对映体富集杂环化合物的总收率高达 78%,对映体比率高达 99:1。