Direct alkenylation of alkylazaarenes with aldehydes through C(sp(3))-H functionalization under catalytic InCl3 activation

作者：Jamal Zaini; Teo Yong Chua^*; Lim Gina Shiyun

来源：Tetrahedron, 2016, 72(17): 2132-2138.

DOI：10.1016/j.tet.2016.03.004

• Aldehydes
• Alkylazaarenes
• C-H functionalization
• Indium
• Lewis acid

Under the influence of InCl3 as a Lewis acid catalyst, a methodology on the C(sp(3))-H functionalization of alkylazaarenes has been demonstrated through the activation of benzylic C-H bonds towards their addition reaction with the appropriate electrophiles. This methodology was chiefly applied in the direct alkenylation of primary and secondary benzylic C-H bonds of alkylazaarenes with aldehydes. A variety of alkenyl products were afforded in generally good yields including the starting alkenyl intermediate used in the synthesis of montelukast and other related molecules.

• 出版日期2016-4-28