) Palladium-catalyzed coupling reactions serve as extremely useful tools for the synthesis of biologically active compounds. We propose to develop more powerful catalysts for these reactions, focusing primarily on complexes that employ bulky, electron-rich P(t-Bu)3 as a ligand. For an array of important carbon-carbon bond-forming processes (e.g., Suzuki, Heck, Stille, and Negishi couplings), we intend to develop: general methods for coupling organic chlorides; versatile catalysts for coupling organic bromides, iodides, and triflates under mild conditions (e.g., at room temperature) and general methods for coupling organic phosphates and tosylates. Although our primary objective is to provide practical catalysts that will be widely applied by synthetic chemists both in basic research and in pharmaceutical/chemical development, we will also pursue mechanistic studies directed at furnishing an improved understanding of the origin of the unusual reactivity of Pd/P(t-Bu)3 in these coupling processes.

Agency
National Institute of Health (NIH)
Institute
National Institute of General Medical Sciences (NIGMS)
Type
Research Project (R01)
Project #
5R01GM062871-04
Application #
6729140
Study Section
Medicinal Chemistry Study Section (MCHA)
Program Officer
Schwab, John M
Project Start
2001-04-01
Project End
2005-03-31
Budget Start
2004-04-01
Budget End
2005-03-31
Support Year
4
Fiscal Year
2004
Total Cost
$279,511
Indirect Cost
Name
Massachusetts Institute of Technology
Department
Chemistry
Type
Schools of Arts and Sciences
DUNS #
001425594
City
Cambridge
State
MA
Country
United States
Zip Code
02139
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