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Pd/PTABS: Catalyst for Room Temperature Amination of Heteroarenes
Siva Sankar Murthy Bandaru1, Shatrughn Bhilare2, Nicolas Chrysochos1
1Institut für Biochemie, Ernst-Moritz-Arndt-Universität Greifswald , Felix-Hausdorff-Str. 4, 17489 Greifswald, Germany.
Abstract:
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.
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