Enantioselective Catalytic Methods for Drug Synthesis

Award Information
Agency:
Department of Health and Human Services
Branch
n/a
Amount:
$50,000.00
Award Year:
1993
Program:
SBIR
Phase:
Phase I
Contract:
n/a
Agency Tracking Number:
22282
Solicitation Year:
n/a
Solicitation Topic Code:
n/a
Solicitation Number:
n/a
Small Business Information
Regis Chemical Company
8210 Austin Avenue, Morton Grove, IL, 60053
Hubzone Owned:
N
Socially and Economically Disadvantaged:
N
Woman Owned:
N
Duns:
n/a
Principal Investigator:
Christopher J. Welch
(708) 967-6000
Business Contact:
() -
Research Institution:
n/a
Abstract
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.

* information listed above is at the time of submission.

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