MSU Technologies

Catalytic Processes for Boronic Esters and Substituted Boranes

Executive Summary

In the pharmaceutical industry, organoboron complexes are key building blocks for drug manufacturing, versatile reagents for high-throughput parallel synthesis in drug discovery and exhibit some useful and unique biological activities. However, conventional synthesis routes can be complex and involve undesirable reagents. MSU researchers have developed processes for efficient synthesis of a wide range of substituted boranes and boronic esters covered by a suite of issued US patents.

Description of the Technology

The technology is covered in a suite of patents that describe processes to make complex polyphenylenes, ring substituted arene boranes, substituted phenols containing aryl or hetroaryl groups, aminoarylboronic esters, cyano ring-substituted arene or heteroarene boranes. The basic technology involves reacting chemical precursors with borane materials in the presence of iridium or rhodium complexes which may be further reacted in the presence of metal catalysts.

Benefits

Low catalyst concentrations
Does not require organolithium reagents, ethereal solvents. Reactions can be carried out neat
Wide range of functional groups possible
High selectivity, avoids costly intermediate purification steps
Allows production of new range of boron containing chemicals which are difficult to synthesize or not available