Study On The Synthesis Of New Indole Boric Acid And Boronic Acid Esters

Indole derivatives are widely found in nature.They are important heterocyclic compounds in fine products such as medicine and pesticide.Organoboronic acids and their derivatives,especially arylboronate esters,are powerful and versatile reagents in synthetic organic chemistry,medicine,and materials science owing to their high stability,low toxicity,and synthetic utility in various transformations.Lithium amide method and format reagent method are the most commonly used methods for the synthesis of organic borides,In this paper,a new preparation method is adopted to prepare indole boric acid compounds through a novel transition metal catalyst..The goal of this research is the synthesis of new indole boric acid compounds,which are mainly changed from C-H bonds to C-B bonds directly through metal iridium catalysts.While the regioselectivity of aromatic C-H borylations is mainly driven by steric effects,this method of boronization does not require the participation of halogen groups,and the amount of catalyst is very small,which is simpler and more effective than the traditional synthesis method.In this paper,a small amount of indole boronic acid ester compound is synthesized by the method of metal palladium catalysis.By examining the reaction conditions and reaction post-treatment operations,18kinds of new indole boronic acids and boric acid esters were synthesized.Among them,there were 16 compounds whose synthesis method needed to be designed by ourselves;There are reports in the literature but the reaction route is more complicated,the yield is lower and the post-processing is cumbersome,there are 2 that need to be improved.Their structures were confirmed by ~1H NMR and MS.