Friedel-Crafts Reaction Of Indoles With Imines By Acids Catalyst

Indole derivatives are a class of Heterocycle, which not only widespread exist in nature ,but also most have potent pharmacological activity, so takeing indole as raw material to synthesize natural products with pharmacological activity or natural product derived compounds to be used for screening purposes has been the core of study for chemical indole. Thus, the research of indole ring derivative method is extremely important. Indole 3- position introduce some new functional group so it easy to derivative. In this way, we can take the product of Friedel-Crafts reaction as reaction intermediates to synthesized intent product. From the existing research result, we have solved the 3 - bit selective indole Friedel-Crafts reaction at some extent, however, Indole Friedel-Crafts reaction of green synthetic methods have yet to be studied in depth. This article is based on the indole Friedel-Crafts reaction, with a view to filter out the mild reaction conditions, simple operation, convenience, and post-processing environment-friendly new indole Friedel-Crafts reaction.In this paper, baseing on the review of research progress of indole ring of 3 -bit regional selective indole Friedel-Crafts reaction, the main work as follows:1. The Perchlorate catalyzed Friedel-Crafts addition of indoles to N-sulfonyl aldimines were developed. and high yield (from 53% to 92%) were achieved. And the structures of the products of Friedel-Crafts reaction were further established by the X-ray diffraction studies.2. The highly yield (51% -95%) addition of indoles to N-AcylImines and N-sulfonyl aldimines with use of a heteropoly acid catalyst. A series of bisindolymethane compounds were mild and efficient synthesized. In the process, heteropoly acid as a cheap easy to get the solid acid catalyst, with a convenient handle, less polluting and many other advantages, for the response to this is a trend in line with the development of modern chemistry green catalyst.These methods are simple, mild reaction conditions, environment-friendly, regional selective specificity, and a good yield.