An Automated-Flow Microreactor for 100g synthesis using the Sonogashira reaction

Chemists at the synthetic chemistry department at Shionogi in Japan have reported the use of an automated microreactor system to quickly optimise the conditions for a complex Sonogashira reaction and to produce 100g quantities in as little as 50 hours (both optimisation and production) –see Sugimoto A et al, (Tet Lett  2009, 50, 6364-7) for more details.  Temperatures of 70, 90 and 110 degrees and residence times of 20, 40 and 60 minutes were evaluated in the first screen, and 110/120 degrees and 10,20 and 40 minutes residence time in the second screen; stoichiometry and amine quantity were investigated in later screens before the optimum conditions were found.

The microreactors used were from Dainippon Screen Mfg Co Ltd and a stainless steel one with a T-shaped microchannel (www.michs.jp).