The proposed research will allow the development of a new novel method for the synthesis of compounds which contain structural elements with known biological activity. A novel asymmetric nitrogen-centered radical cyclization on to a tethered olefin is proposed. The ability to strategically place a chiral auxiliary directly adjacent to the prochiral radical A or next to the olefin B should allow for a significant amount of asymmetric induction. The proposed method will be developed for the formation of 4 - 6 membered nitrogen containing heterocycles. Most importantly, this new methodology provides an easy route for the synthesis of a large number of analogs of the known therapeutic agents. Also with this new method, one could envision the ability to catalog large numbers of structurally similar compounds to be evaluated for biological activity as well. The ability to synthesize and test these new compounds provides the potential to enhance the already proven activity while minimizing toxic side effects and maintaining therapeutic value. Of particular interest is the synthesis of compounds which display a significant amount of antitumor activity.

Agency
National Institute of Health (NIH)
Institute
National Institute of General Medical Sciences (NIGMS)
Type
Postdoctoral Individual National Research Service Award (F32)
Project #
1F32GM019021-01A1
Application #
2639748
Study Section
Medicinal Chemistry Study Section (MCHA)
Project Start
1998-09-30
Project End
Budget Start
1998-05-01
Budget End
1999-04-30
Support Year
1
Fiscal Year
1998
Total Cost
Indirect Cost
Name
Scripps Research Institute
Department
Type
DUNS #
City
La Jolla
State
CA
Country
United States
Zip Code
92037