Enantioselective Catalytic Methods for Drug Synthesis
A new family of enantioselective dirhodiumn(II) catalysts have been developed by Professor Michael P. Doyle at Trinity University using a rational approach employing molecular modeling and molecular orbital calculations. These catalysts show an extraordinary ability to enantioselectively catalyze a number of different organic reactions, allowing the convenient synthesis of a number of otherwise difficult to obtain enantioenriched materials. These catalysts are excellent candidates for commercialization, showing high yields, enantioselectivities, and turnover numbers, and a degree of ruggedness which permits catalyst recovery and reuse. The specific aims for Phase I are (1) To transfer the technology for catalyst production and use from the Doyle laboratories to Regis, and to prepare scaled up quantities of the catalysts Rh2(5R-MEPY)4 and Rh2(5S-MEPY)4 for use in application studies, (2) to use these catalysts to prepare selected products of cyclopropanation and intramolecular C-H insertion reactions, and (3) to use chiral chromatography as a tool to upgrade the products of these reactions from high enantioenrichm- ent to enantiopurity. Phase I and Phase II grants will provide an opportunity to demonstrate the utility of the Doyle technology for the commercial production of highly useful enantiopure organic intermediates and pharmaceutical products.
Small Business Information at Submission:
Principal Investigator:Christopher J. Welch
Regis Chemical Company
8210 Austin Avenue Morton Grove, IL 60053
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