Single Step Method for Heterocycle Synthesis

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2018-DAI-68010
N-heterocycles are contained in more than half of FDA-approved small-molecule therapeutics. These heterocycles are highly important for the development of new therapeutics. However, several heterocycles are difficult to access, and there is a significant lack of structural diversity of the heterocycles due to lack of efficient and limited methods to synthesize N-heterocycles. Therefore, there is need of a method for synthesizing heterocycles efficiently.

Researchers at Purdue University have developed a novel strategy for rapidly synthesizing carbon-substituted heterocycles in one step. The reactions in the approach are optimized and utilize reagents that are cheap and readily available, eliminating the need for precious transition metal catalysts. In addition, products can be converted to more complex products, improving structural diversity further. This technology for producing nitrogen-containing heterocycles would help in numerous applications, including medicinal chemistry and the therapeutic drug discovery/development process.

Advantages:
-Single step
-Inexpensive
-Optimized reactions
-Improved structural diversity

Potential Applications:
-Medicinal chemistry
-Drug discovery
-Therapeutic development
Jul 13, 2018
Utility Patent
United States
10,800,745
Oct 13, 2020

Aug 11, 2020
DIV-Gov. Funding
United States
(None)
(None)

Aug 18, 2017
Provisional-Patent
United States
(None)
(None)
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