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SBIR Phase I:Ring Contraction Metathesis Reaction for the Generation of Novel…

Award Information

Agency:
National Science Foundation
Branch:
N/A
Award ID:
98750
Program Year/Program:
2010 / SBIR
Agency Tracking Number:
0943648
Solicitation Year:
N/A
Solicitation Topic Code:
CT8
Solicitation Number:
N/A
Small Business Information
MCP
200 Boston Ave suite 4750 Medford, MA 02155-4258
View profile »
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 1
Fiscal Year: 2010
Title: SBIR Phase I:Ring Contraction Metathesis Reaction for the Generation of Novel Polyene Macrolides
Agency: NSF
Contract: 0943648
Award Amount: $144,579.00
 

Abstract:

This Small Business Innovation Research (SBIR) Phase I project will develop a process for modifying macrolide natural products in general and Rapamycin in particular using a relatively new chemical transformation called the ring contraction metathesis reaction. The modified compounds will contain a novel contracted core that is inaccessible by conventional methods in a cost effective way. Rapamycin is an immunosuppressant used widely in transplantation, autoimmune and oncological diseases and drug coated stents. The major draw back of rapamycin is its extremely long half-life (63h) which leads to tolerability issues. The novel synthetic transformation outlined in this Phase I Research will allow for the synthesis of a novel new rapamycin analogs with improved pharmacological properties, such as shorter half-life. The broader impacts of this research are the following: First, development of this reaction into a general synthetic process will allow for the generation of a variety of new and novel compounds which cannot be prepared in any other way. The ring contraction process will generate novel natural product structures that could function as new chemical probes to better understand biological processes. Furthermore, novel macrolide compounds could advance national health concerns by providing new drugs with an improved therapeutic profile. Secondly, the generation of novel Rapamycin analogs will improve the health and quality of life of organ transplant patients as well as form the basis for ongoing research in oncology and auto immune diseases.

Principal Investigator:

steven W. riesinger
DPhil
7813960476
sriesinger@medchempartners.com

Business Contact:

steven W. riesinger
DPhil
7813960476
sriesinger@medchempartners.com
Small Business Information at Submission:

MCP
200 Boston Ave suite 4750 Medford, MA 02155

EIN/Tax ID: 204822217
DUNS: N/A
Number of Employees:
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No