Automated Synthesizer for Small Molecules

As reported on the Howard Hughes Medical Institute’s web site:

Scientists led by Martin Burke, an HHMI early career scientist at the University of Illinois at Urbana-Champaign, used a single automated process to synthesize 14 distinct classes of small molecules from a common set of building blocks. Burke’s team envisions expanding the approach to enable the production of thousands of potentially useful molecules with a single machine, which they describe as a “3D printer” for small molecules. Their work is described in the March 13, 2015, issue of the journal Science.

According to Burke, the highly customized approach that chemists have long relied on to synthesize small molecules is time consuming and inaccessible to most researchers. “A lot of great medicines have not been discovered yet because of this synthesis bottleneck,” he says. With his new technology, Burke aims to change that. “The vision is that anybody could go to a website, pick the building blocks they want, instruct their assembly through the web, and the small molecules would get synthesized and shipped,” Burke says. “We’re not there yet, but we now have an actionable roadmap toward on-demand small-molecule synthesis for non-specialists.”

While “3D printer” is a bit of an exaggeration, conceptually this is a very powerful technique.  The method (which, it can’t be over emphasized, is still in it’s infancy) takes molecular building blocks with connectors on either end and then “prints” them out in any combination you specify.  The real breakthrough is more along the lines of the digitization of chemistry, and a better analogy might be the way DNA synthesis is done currently.  DNA synthesis used to be done by hand in a chemistry lab but is now done in incredibly high throughput on automated synthesizers.  By commoditizing and miniaturizing small molecule chemical synthesis in a similar way, vast amounts of synthesis could be done very fast and very cheaply.

One limitation of the method is the small scale of the reactions, but scientist are working on solutions for that, too.