Despite its advances, small molecule synthesis still remains a complex, unsystematized, and time-intensive process. As a result, it is practiced almost exclusively by highly trained specialists. Collectively, these limitations represent a major bottleneck in efforts to study the functional capacity of small molecules. In an effort to shift the rate-limiting step of small molecule science from synthesis to function study, we have constructed a fully automated synthesizer that uses only the Suzuki-Miyaura cross-coupling reaction, in an iterative fashion, to assemble off-the-shelf building blocks into many different types of small molecules, including organic materials, pharmaceuticals, natural products, and natural product derivatives. With thousands of applicable building blocks commercially available or easily accessible, this now simple, general, and fully automated synthesis platform stands to afford more efficient access to targets to specialists and non-specialists alike.

Automated iterative cross-coupling for the synthesis of diverse small molecules

246th National Meeting (2013)

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