The goal of the Phase II SBIR is to conduct research and development that will allow Fluorous Technologies, Inc. to ramp up from current analytical/demonstration libraries to the actual production of libraries of a size and scale that will be attractive to pharmaceutical and biotechnology companies. Once this capability is in place, FTI intends to be a highly competitive player in the outsourcing market for combinatorial library synthesis. This market is currently estimated at $145 million for 2000, with an annual growth rate of 15%. In addition, the technology will also be commercialized for external use. Building on successful Phase I work, the grant proposes the synthesis of 4,800-9,600 member library of mappicine analogs on 2-3 mg scale using the company's innovative new """"""""fluorous mixture synthesis"""""""" platform. The work is divided into the """"""""preparation phase"""""""", where all the needed starting materials, fluorous tags, and diversity reactants will be prepared, and the """"""""production phase"""""""", where the library will be produced, purified and analyzed.

Proposed Commercial Applications

The research will validate FTI's fluorous mixture synthesis techniques in a real world setting. The company plans to use the techniques in- house for contract library synthesis and to make them available to the community at large.

Agency
National Institute of Health (NIH)
Institute
National Institute of General Medical Sciences (NIGMS)
Type
Small Business Innovation Research Grants (SBIR) - Phase II (R44)
Project #
2R44GM062717-02
Application #
6485131
Study Section
Special Emphasis Panel (ZRG1-SSS-L (10))
Program Officer
Schwab, John M
Project Start
2001-04-10
Project End
2004-03-31
Budget Start
2002-04-01
Budget End
2004-03-31
Support Year
2
Fiscal Year
2002
Total Cost
$960,248
Indirect Cost
Name
Fluorous Technologies, Inc.
Department
Type
DUNS #
010561103
City
Pittsburgh
State
PA
Country
United States
Zip Code
15238
Zhang, Wei (2007) Fluorous-enhanced multicomponent reactions for making drug-like library scaffolds. Comb Chem High Throughput Screen 10:219-29
Chu, Qianli; Yu, Marvin S; Curran, Dennis P (2007) New fluorous/organic biphasic systems achieved by solvent tuning. Tetrahedron 63:9890-9895
Lu, Yimin; Zhang, Wei (2006) Fluorous 2,4-Dichloro-1,3,5-triazines (F-DCTs) as Nucleophile Scavengers. QSAR Comb Sci 25:728-731
Zhang, Wei (2006) Microwave-Enhanced High-Speed Fluorous Synthesis. Top Curr Chem 266:145-166
Zhang, Wei; Nagashima, Tadamichi (2006) Palladium-Catalyzed Buchwald-Hartwig Type Amination of Fluorous Arylsulfonates. J Fluor Chem 127:588-591
Zhang, Wei; Lu, Yimin (2006) Fluorous 2,4-Dichloro-1,3,5-triazine (F-DCT) as Amide Coupling Agent. QSAR Comb Sci 25:724-727
Zhang, Wei; Lu, Yimin; Chen, Christine Hiu-Tung et al. (2006) Fluorous Synthesis of Hydantoin-, Piperazinedione-, and Benzodiazepinedione-Fused Tricyclic and Tetracyclic Ring Systems. European J Org Chem :2055-2059
Zhang, Wei; Lu, Yimin; Hiu-Tung Chen, Christine et al. (2006) Fluorous mixture synthesis of two libraries with hydantoin-, and benzodiazepinedione-fused heterocyclic scaffolds. J Comb Chem 8:687-95
Zhang, Wei (2005) Microwave-Enhanced Fluorous Synthesis. Chim Oggi 23:11-13
Nagashima, Tadamichi; Zhang, Wei (2004) Solution-phase parallel synthesis of an N-alkylated dihydropteridinone library from fluorous amino acids. J Comb Chem 6:942-9

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