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STTR Phase I: Semisynthetic Manufacturing of Core Natural Triterpenoids from Outer Birch Bark Extract

Award Information
Agency: National Science Foundation
Branch: N/A
Contract: 1549685
Agency Tracking Number: 1549685
Amount: $225,000.00
Phase: Phase I
Program: STTR
Solicitation Topic Code: CT
Solicitation Number: N/A
Solicitation Year: 2015
Award Year: 2016
Award Start Date (Proposal Award Date): 2016-01-01
Award End Date (Contract End Date): 2016-12-31
Small Business Information
4505 County Road 92
Waconia, MN 55387
United States
DUNS: 065321915
HUBZone Owned: No
Woman Owned: No
Socially and Economically Disadvantaged: No
Principal Investigator
 Brian Garhofer
 (612) 669-8581
Business Contact
 Brian Garhofer
Phone: (612) 669-8581
Research Institution
 University of Minnesota Duluth
 Pavel A Krasutsky
1049 University Drive
Duluth, MN 55812
United States

 Nonprofit College or University

The broader impact/commercial potential of this Small Business Innovation Technology Transfer Research Phase I project is to facilitate the manufacturing and commercialization of natural and semi-synthetic products namely core lupane triterpenoids (betulin, betulinic acid, lupeol, betulinic aldehyde) as precursors for drug development and other industrial applications. Research shows that these triterpenoids can be useful agents for prevention and treatment of cancer, chronic inflammation, HIV/AIDS, type 2 diabetes, tuberculosis, metabolic disease, as well as next generation antimicrobials, and vaccine adjuvants. Unfortunately, the complex isolation and/or chemical synthesis of these compounds has resulted in low scale yields at costs of more than US$10,000/kg. The fundamental potential of this project lies in the demonstration of the use of certain selective organic reactions to produce these high value compounds straight from the complex composition of the natural extract found in the outer bark of the birch tree, a renewable, natural resource found extensively throughout the northern climates. This approach is novel and if successful, can result in significantly higher yields while eliminating multiple complex synthesis steps, thus providing a large diversity of triterpenoids that were previously not available in commercial quantities. The technical objective in Phase I research project is the development of a principally new way of pure natural and semi-synthetic chemical manufacturing from the triterpenoid extract found in the outer bark of the birch tree. The specific objectives of this project are to develop the methods and processes to 1) provide commercial quantities of outer bark, free from impurities and foreign matter, 2) develop the processes to extract the natural triterpenoids (BBE) from the outer bark and remove unwanted contaminants. 3) Develop the synthesis processes to convert the triterpene extract to the semi-synthetic precursors necessary with the quality and purity to be used for drug development. This research will provide specially designed processes of bark screening, separation and densification to provide a pure material that can be efficiently and economically processed. Extraction methods will be developed to remove traces of tannins, pigments, suberin, and other unwanted materials. Innovative new ways for the straight semisynthetic production of the triterpenoids directly from BBE, will be developed to lead to the creation of a large scale production process for triterpenoids as fine chemicals.

* Information listed above is at the time of submission. *

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