THE PROPOSED PROGRAM RELATES TO THE SYNTHESIS OF (13)C MULTILABELED CHOLESTEROL AND -SITOSTEROL AS POTENTIAL DIAGNOSTIC AGENTS.

Award Information
Agency:
Department of Health and Human Services
Branch
n/a
Amount:
$49,979.00
Award Year:
1984
Program:
SBIR
Phase:
Phase I
Contract:
n/a
Award Id:
1538
Agency Tracking Number:
1538
Solicitation Year:
n/a
Solicitation Topic Code:
n/a
Solicitation Number:
n/a
Small Business Information
Tracer Technologies Inc. (Currently ECO ENERGY CONVERSION)
225 Needham Street, Newton, MA, 02164
Hubzone Owned:
N
Minority Owned:
N
Woman Owned:
N
Duns:
n/a
Principal Investigator:
SUN SHINE YUAN
PRINCIPAL SCIENTIST
() -
Business Contact:
() -
Research Institution:
n/a
Abstract
THE PROPOSED PROGRAM RELATES TO THE SYNTHESIS OF (13)C MULTILABELED CHOLESTEROL AND -SITOSTEROL AS POTENTIAL DIAGNOSTIC AGENTS. HYPERCHOLESTEROLEMIA HAS BEEN IMPLICATED AS A PRIMARY RISK FACTOR IN CORONARY HEART DISEASE YET MAJOR QUESTIONS REGARDING CHOLESTEROL ABSORPTION, TRANSPORT, REVERSE TRANSPORT AND DISPOSITION REMAIN TO BE ELUCIDATED FOR LACK OF A SAFE, CONVENIENT NON-RADIOACTIVE TRACER METHODOLOGY. THUS, STABLE ISOTOPE LABELED DIETARY STEROLS IN CLINICAL PROTOCOLS, COMBINED WITH MASS FRAGMENTOGRAPHY, CAN BE EXPECTED TO AID THE ELABORATION OF INDECES FOR SUCH PARAMETERS AS STEROL POOL SIZE, TRANSIT TIME, VOLUME DISTRIBUTION AND CLEARANCE. THE SYNTHETIC APPROACH REQUIRES DISCONNECTION AT C-22 OF THE STEROL SIDE CHAIN AND RESYNTHESIS WITH THE LABELS POSITIONED IN THE ISOPROPYL TERMINUS AT (C-25, 26 AND 27), THE LATTER BEING DERIVED FROM (13)C3-ACETONE. INCLUDED AMONG THE PROJECT TASKS ARE DEVELOPMENT OF PATHWAYS CONSERVATIVE TOWARDS ISOTOPE AND OPTIMIZATION OF YIELDS TO PROVIDE MULTIGRAM QUANTITIES OF BOTH STEROLS IN SEVEN SYNTHETIC STEPS. YIELDS IN THE 10-20% RANGE ARE EXPECTED. ADDITIONALLY, THE PROGRAM CALLS FOR DEVELOPMENT OF AN A-RING DEGRADATION AND RESYNTHESIS VIA THE ROBINSON ANNELATION TO GIVE (13)C4-LABELED STEROLS. A REPERTORY OF VARIOUS INCREMENTALLY LABELED A AND/OR CHAIN LABELED STEROLS CAN THEN BE ENVISIONED FOR APPLICATION IN SIMULTANEOUS STUDIES BY MULTIPLE ROUTES OF TRACER ADMINISTRATION.

* information listed above is at the time of submission.

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