Pd/PTABS: Catalyst for Room Temperature Amination of Heteroarenes,Organic Letters

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Pd/PTABS: Catalyst for Room Temperature Amination of Heteroarenes
Organic Letters ( IF 4.9 ) Pub Date : 2018-01-05 00:00:00 , DOI: 10.1021/acs.orglett.7b03854
Siva Sankar Murthy Bandaru ₁ , Shatrughn Bhilare ₂ , Nicolas Chrysochos ₁ , Vijay Gayakhe ₂ , Ivan Trentin ₁ , Carola Schulzke ₁ , Anant R. Kapdi ₂

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A mild and highly efficient catalytic amination procedure for chloroheteroarenes at ambient temperature using the Pd/PTABS catalytic system is reported. The protocol is selective for the amination of chloroheteroarenes using secondary amines such as piperidine, pyrrolidine, and several others. The exceptional mildness of the developed protocol is beneficial for the synthesis of a crucial Buparlisib intermediate as well as the formal synthesis of Alogliptin in competitive yields.

中文翻译：

Pd / PTABS：杂芳烃室温胺化的催化剂

据报道，在室温下使用Pd / PTABS催化体系进行的氯杂芳烃温和高效的催化胺化程序。该方案对于使用仲胺（例如哌啶，吡咯烷和其他几种胺）进行氯杂芳烃的胺化反应具有选择性。所开发方案的非凡温和性，对于关键的布氏替尼中间体的合成以及以竞争性收率进行阿格列汀的正式合成都是有益的。

更新日期：2018-01-05

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