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
Applications
- Drug manufacturing
- Reagents for complex chemical synthesis
- Chemical building blocks
Patent Status
US 7,148,356, US 7,329,769, US 6,828,466, US 6,958,420, US 7,514,563
Licensing Rights
Non exclusive licensing rights available
Inventors
Dr. Milton Smith, Dr. Robert Maleczka, Dr. Daniel Holmes, Dr. Feng Shi, Dr. Ghayoor A. Chotana
TECH ID
TEC2001-0053, TEC2003-0005, TEC2003-0006, TEC2005-0112
