A Novel Synthesis Method of Meriolin1

Abstract

Meriolins, a compound designed and synthesized by the similar structure of natural marine products Meridianins and Variolins, has been proved to be a new kinase inhibitor that can enhance protein kinase selectivity and cell death. It has stronger inhibitory activity, relative selectivity to kinases and antitumor effect. As the first compound in the Meriolins series, Meriolin1 has been studied the most. In this paper, the synthesis methods of Meriolin1 at home and abroad were summarized and analyzed. On this basis, a more economical and effective synthesis route was designed, that is, Meriolin1 was finally obtained from 7-azaindole through Friedel-crafts acylation, protection, aldol condensation and cyclization reaction. This route avoids the disadvantages of the existing routes and has the advantages of mild reaction conditions, simple operation and low cost. The structures of the compounds were confirmed by 1H NMR and 13C NMR.