Awardee OrganizationBOSTON UNIVERSITY MEDICAL CAMPUS
Description
Abstract Text
The specific aim of this investigation is to explore and develop the
chemistry of Alpha-oxoketene dithioacetals. Two procedures are being
developed for the efficient exploitation of this functional group for
selective (i.e. chemoselective, regioselective and stereoselective)
carbon-carbon bond constructions and functional group manipulations. The
first method involves the chemoselective and stereoselective conjugate
addition of organocuprates to Alpha-oxoketene dithioacetals and to the
resultant vinylogous thioesters. The second method involves
1,2-nucleophilic additions to the ketone carbonyl followed by acid
catalyzed rearrangement and constitutes a versatile 1,3-carbonyl
transposition methodology that permits regioselective sequential
carbon-carbon bond constructions. The specific goals are two-fold. First,
the scope, limitations, and reaction parameters of these two procedures
will be examined in very careful detail. Second, the synthetic application
of this chemistry to the synthesis of Alpha-alkylidene ketones,
Alpha-pyrones, and simple and annulated benzene derivatives will be
examined. Development of these methodologies will provide general routes
to several classes of compounds and will provide versatility for the
construction of specific substitution patterns. Each of the synthetic
applications will require studies to optimize reaction conditions and
determine the scope and limitations of the synthetic routes. The
development of methods for the sequential regio-, stereo-, and
chemoselective construction of new carbon-carbon bonds utilizing the
Alpha-oxoketene dithioacetal cascade will provide versatile synthetic
opportunities. In preliminary work the power of these synethetic methods
has been illustrated by a total synthesis of Myodesmone. The direct entry
into the rich chemistry of regio- and stereospecifically substituted
allylic alcohols provides another example.
The development of methods for the synthesis of heterocycles (e.g.
Alpha-pyrones) and benzenoid aromatic compounds will contribute to the
search for active medicinal compounds. The methodologies are applicable to
the synthesis of biologically active natural products and synthetic
medicinals.
No Sub Projects information available for 1R01GM031776-01A1
Publications
Publications are associated with projects, but cannot be identified with any particular year of the project or fiscal year of funding. This is due to the continuous and cumulative nature of knowledge generation across the life of a project and the sometimes long and variable publishing timeline. Similarly, for multi-component projects, publications are associated with the parent core project and not with individual sub-projects.
No Publications available for 1R01GM031776-01A1
Patents
No Patents information available for 1R01GM031776-01A1
Outcomes
The Project Outcomes shown here are displayed verbatim as submitted by the Principal Investigator (PI) for this award. Any opinions, findings, and conclusions or recommendations expressed are those of the PI and do not necessarily reflect the views of the National Institutes of Health. NIH has not endorsed the content below.
No Outcomes available for 1R01GM031776-01A1
Clinical Studies
No Clinical Studies information available for 1R01GM031776-01A1
News and More
Related News Releases
No news release information available for 1R01GM031776-01A1
History
No Historical information available for 1R01GM031776-01A1
Similar Projects
No Similar Projects information available for 1R01GM031776-01A1