Mettler-Toledo Webinar on Ugi Reaction

I am presenting a webinar courtesy of Mettler-Toledo tomorrow - Optimization of a Ugi Reaction Using MiniBlock® - presented by Dr. Jean-Claude Bradley of Drexel University taking place tomorrow, Tuesday, September 23 at 9am and 2pm US EDT. If you have not already registered, click here. (See related Nature Precedings report)

The Ugi reaction involves the mixing of four components: an aldehyde, an amine, a carboxylic acid, and an isonitrile. The Ugi reaction is a convenient reaction to generate diverse libraries and has been used in the past to generate antimalarial compounds. The particular Ugi reaction that we consider involves the reaction of furfurylamine, benzaldehyde, boc-glycine and t-butylisonitrile. This reaction produces a Ugi product as a precipitate when run at 0.5M concentration in methanol. We will describe the optimization of this reaction by varying the solvent, concentration, and excess of some reagents.

This webinar will last for 30 minutes and at the end there will be an interactive Q&A session providing you with the opportunity to ask questions relevant to your particular application.

Register for the webinar on Tuesday, September 23.

Laboratory Automation Talk at Drexel

Tom Osborne from Mettler-Toledo will give a talk on laboratory automation at 10:30 a.m. on Tuesday July 1, 2008 in Disque 109 (32^nd and Chestnut streets).

The presentation will focus on chemistry applications of the MiniBlock, MiniBlock XT, and MiniMapper systems, including some results from the Bradley lab on the optimization of the Ugi reaction. A laboratory demonstration will follow in Disque 511.

RSVP Jean-Claude.Bradley@drexel.edu to attend.

MiniBlock® is a flexible, easy to use tool designed for parallel synthesis. MiniBlock® is the only compact parallel synthesizer that allows synthesis via Solid Phase or Solution Phase to be carried out on the same platform. Originally designed by medicinal and combinatorial chemists at Bristol-Myers Squibb Company, the MiniBlock® has been further developed to address a wide range of chemistry methodologies.

MiniMapper in Lab

As I mentioned previously, Mettler-Toledo is giving us a trial with their MiniMapper/MiniBlock system. Tom Osborne was in my lab yesterday to set it up. We got as far as setting up the software to recognize the positions of bottles and racks and pumping through some methanol.


Once we're set up it looks like we'll be able to come pretty close to just copying columns from the Google spreadsheet of planned experiments to the MiniMapper software. This will make it very convenient for crowdsourcing Ugi experiments.

Actually the worksheet for trial #3 is already set up to accept suggested experiments from anyone - no login required. Just note your name in the contributor column and put in a little explanation for your reasoning. For example, after looking at the master table of Ugi reactions, you may have a hypothesis that aromatic aldehydes lead to Ugi product precipitates at 0.5 M concentration in methanol. Just set up a dozen experiments probing that question. See the MettlerTrial wiki page for more info. I'll explain more about this later but if anyone wants to discuss collaboration contact me.

We have the capacity of doing 96 experiments in parallel but Khalid will probably start with a dry run with pure methanol or a small section from Trial #1.

Tom made a good point about how organic chemists need to think differently when designing experiments in parallel with automation. We have done parallel runs in vials but it gets tricky for people to keep track of everything. Machines are much better at this type of thing. You have to ask different questions when faced with 96 reaction tubes vs. a round-bottomed flask.

And it looks like the MiniMapper software keeps a log in XML format - obviously more on that after our first trial...