EXCEED THE SPACE PROVIDED. Ayest apofowuenrfdualtionmethuopdosn wfohricthe nseywnthmeseidsicinoafl coaregenotrsganciacn fbuencctionsatlriutiectse,d, asit wiselilmpaosrtmanetthotdos untchoavteralloswimptlhee, core structures to be easily substituted with a wide variety of substituents. It is in support of health sciences in general that the chemistry proposed within finds its significance. Because of the unique ability of transition metal species to effect the formation of carbon-carbon and carbon-heteroatom bonds under very mild conditions, emphasis in this proposal is placed on the use of organotransition metal chemistry to facilitate a variety of transformations. An underlying theme of the )roposed chemistry is the development of flexible new synthetic methods that will facilitate the structure-activity-relationship studies that lead to the discovery of new medicinal agents. PERFORMANCE SITE(S) (organization, city, state) Emory University Department of Chemistry 1515 Pierce Drive Atlanta, Georgia 30322 KEY PERSONNEL. See instructions. Use continuation pages as needed to provide the required information in the Start with Principal Investigator. List all other key personnel in alphabetical order, last name first. Name Organization Liebeskind, Lanny S. Emory University Srogl, Jiri Emory University Disclosure Permission Statement. Applicable to SBIR/STTR Only. See instructions. [] Yes [] No PHS 398 (Rev. 05/01) Page 2 Number pages consecutively at the bottom throughout the application. Do no._u_sLet suffixessuch as 3a, 3b. format shown below. Role on Project Principal Investigator St. Research Associate Form Page 2 ========================================Section End===========================================

Agency
National Institute of Health (NIH)
Institute
National Institute of General Medical Sciences (NIGMS)
Type
Research Project (R01)
Project #
5R01GM066153-21
Application #
6834570
Study Section
Medicinal Chemistry Study Section (MCHA)
Program Officer
Schwab, John M
Project Start
1998-03-20
Project End
2006-12-31
Budget Start
2005-01-01
Budget End
2005-12-31
Support Year
21
Fiscal Year
2005
Total Cost
$262,147
Indirect Cost
Name
Emory University
Department
Chemistry
Type
Schools of Arts and Sciences
DUNS #
066469933
City
Atlanta
State
GA
Country
United States
Zip Code
30322
Varela-Alvarez, Adrian; Liebeskind, Lanny S; Musaev, Djamaladdin G (2012) Mechanistic Insights into the Aerobic Cu(I)-Catalyzed Cross-Coupling of S-Acyl Thiosalicylamide Thiol Esters and Boronic Acids. Organometallics 31:7958-7968
Li, Hao; He, Anyu; Falck, John R et al. (2011) Stereocontrolled synthesis of ?-amino-?'-alkoxy ketones by a copper-catalyzed cross-coupling of peptidic thiol esters and ?-alkoxyalkylstannanes. Org Lett 13:3682-5
Zhang, Zhihui; Lindale, Matthew G; Liebeskind, Lanny S (2011) Mobilizing Cu(I) for carbon-carbon bond forming catalysis in the presence of thiolate. Chemical mimicking of metallothioneins. J Am Chem Soc 133:6403-10
Wu, Wenting; Zhang, Zhihui; Liebeskind, Lanny S (2011) In situ carboxyl activation using a silatropic switch: a new approach to amide and peptide constructions. J Am Chem Soc 133:14256-9
Musaev, Djamaladdin G; Liebeskind, Lanny S (2009) On the Mechanism of Pd(0)-Catalyzed, Cu(I) Carboxylate-Mediated Thioorganic-Boronic Acid Desulfitative Coupling. A Non-innocent Role for Carboxylate Ligand. Organometallics 28:4639-4642
Zitomer, Nicholas C; Mitchell, Trevor; Voss, Kenneth A et al. (2009) Ceramide synthase inhibition by fumonisin B1 causes accumulation of 1-deoxysphinganine: a novel category of bioactive 1-deoxysphingoid bases and 1-deoxydihydroceramides biosynthesized by mammalian cell lines and animals. J Biol Chem 284:4786-95
Liebeskind, Lanny S; Yang, Hao; Li, Hao (2009) A copper-catalyzed, pH-neutral construction of high-enantiopurity peptidyl ketones from peptidic s-acylthiosalicylamides in air at room temperature. Angew Chem Int Ed Engl 48:1417-21
Li, Hao; Yang, Hao; Liebeskind, Lanny S (2008) Synthesis of high enantiopurity N-protected alpha-amino ketones by thiol ester-organostannane cross-coupling using pH-neutral conditions. Org Lett 10:4375-8
Liu, Songbai; Liebeskind, Lanny S (2008) A simple, modular synthesis of substituted pyridines. J Am Chem Soc 130:6918-9
Zhang, Zhihui; Yu, Ying; Liebeskind, Lanny S (2008) N-amidation by copper-mediated cross-coupling of organostannanes or boronic acids with o-acetyl hydroxamic acids. Org Lett 10:3005-8

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