The incorporation of additional Csp3 atoms into candidate drugs may enhance their pharmacological properties.Nevertheless,it remains challenging to construct desired Csp3-Csp3 bonds efficiently and practically.The pre...The incorporation of additional Csp3 atoms into candidate drugs may enhance their pharmacological properties.Nevertheless,it remains challenging to construct desired Csp3-Csp3 bonds efficiently and practically.The present article reports a novel Csp3-Csp3 bond-forming reaction of 2-aryl/alkyl substituted aziridines with gem-diborylalkanes under tranisiton metal free conditions.A wide range ofγ-gem-diboronate esters substituted amines can be accessed in good yield and regioselectivity.The results demonstrated that various aziridines could react with gem-diborylalkanes in the presence of LiTMP as the base within 15 min at ambient temperature.展开更多
基金financial support provided by the National Natural Science Foundation of China(No.22001203).
文摘The incorporation of additional Csp3 atoms into candidate drugs may enhance their pharmacological properties.Nevertheless,it remains challenging to construct desired Csp3-Csp3 bonds efficiently and practically.The present article reports a novel Csp3-Csp3 bond-forming reaction of 2-aryl/alkyl substituted aziridines with gem-diborylalkanes under tranisiton metal free conditions.A wide range ofγ-gem-diboronate esters substituted amines can be accessed in good yield and regioselectivity.The results demonstrated that various aziridines could react with gem-diborylalkanes in the presence of LiTMP as the base within 15 min at ambient temperature.
