Study On The1-position Dierect Arylation And Alkylation Of Isoquinoline Derivatives

Isoquinoline skeleton widely exists in bioactive substances, has been used in the medical field. This kind of frame is also very important intermediates in organic synthesis. Therefore, the synthesis of these compounds has been one of hot topic in the field of organic synthesis workers.This paper mainly divided into two perts:1) A one-pot two-step reaction of2-alkynylbenzaldoximes with aryl halides has been developed, which offers the1-position arylated1,3-disubstituted isoquinoline N-oxides in moderate to good yields in most cases. The isoquinoline N-oxide intermediate was prepared in situ without isolation.2) AgOTf-catalyzed one-pot reactions of2-alkynylbenzaldoximes with various α,β-unsaturated carbonyl compounds under mild conditions are described, which provides a facile and efficient pathway for the synthesis of1-alkylated isoquinoline derivatives.The method tolerates a wide range of substrates and allows for the preparation of the products of interest in moderate to excellent yields.The two reaction protocols show good functional group tolerance and the advantages of mild reaction condition, simple operation, cheap and efficient.