Preparation method of 2-phenylindole derivatives and application thereof

Abstract

The present invention discloses a preparation method and application of 2-phenylindole derivatives. Palladium acetate and copper acetate are added into a glacial acetic acid solution of an indole derivative (formula I) and an arylphenylboronic acid derivative (formula II), stirred at room temperature, and purified to obtain a 2-phenylindole derivative (formula III). The present invention provides a method for direct one-step synthesis of 2-arylindole compounds from indole derivatives and arylphenylboronic acid derivatives as raw materials. The present invention replaces oxygen with air to participate in an oxidation system, expands substituents of indole ring R1, adds substitution of 5-bit, 6-bit and 7-bit electron withdrawing groups and electron donating groups, further expands the range of substrates, and increases the yield of substitution on indole ring R1 by about 13%, wherein 2-methyl and 3-methoxy substituted by R2 and 6-chlorine substituted by R1 have good antifungal activity.

Dependencies are inferred from the claim text.