Abstract
Described here is a concise and modular asymmetric synthesis of N-aryl-2,6-disubstituted piperazine via a Pd-catalyzed carboamination reaction. The process allows the stereoselective preparation of piperazine derivatives with different N1, C2, N4 and C6 groups starting from commercial amino acids. A 4:1 ratio of Pd2(dba)3 and P(2-furyl)3 was found to be the best catalyst system in order to suppress the formation of the major side products B and C. Aryl bromides containing EWG and EDG were found to be effective coupling partners.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have