Synthesis of Natural-Product-Like Molecules with Over Eighty Distinct Scaffolds
2008

Synthesis of Diverse Natural-Product-Like Molecules

publication Evidence: high

Author Information

Author(s): Morton Daniel Leach, Stuart Cordier, Christopher Warriner, Stuart Nelson

Primary Institution: University of Leeds

Hypothesis

Can we create a library of small molecules with high scaffold diversity using a combinatorial approach?

Conclusion

The study successfully developed a method to synthesize over eighty distinct molecular scaffolds, demonstrating high structural diversity.

Supporting Evidence

  • The study created a library of 96 products with distinct molecular scaffolds.
  • High-throughput screens of the synthesized libraries provided useful tools for chemical genetic studies.
  • Approximately 65% of the deprotected scaffolds were novel and not previously prepared.

Takeaway

The researchers figured out how to make a lot of different tiny molecules that look like natural products using a clever method.

Methodology

The study used a combinatorial approach involving the attachment of unsaturated building blocks to a fluorous-tagged linker and employed metathesis reactions to create diverse scaffolds.

Limitations

Some reactions did not proceed to completion, and yields varied widely.

Digital Object Identifier (DOI)

10.1002/anie.200804486

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