High-throughput at Pfizer

01 February 2018 - Orgo

pfizer 2018.PNGNews from Pfizer Worldwide Research and Development! Perera et al. promise 1500 organic reactions per day at nanomole scale and write about it in Science (doi). The work is an extension of automation efforts by competitor Merck who managed 1500 plus reactions in 2.5 hours in 2014 (hello academia?)

The automated unit is massive (see suppl. info for pics): a reaction segment preparation unit can fill up 2 x 96 well-plates with stock solutions using an autosampler (0.5 to 100 microliter dosing, micro-stir bars). These reaction segments are fed into a flow reactor after a solvent selection valve capable of handling 12 different solvents. Each candidate is queued in the flow-reactor coil (100°C, 1 ml/min)and separated by 45 seconds, two LC-MS units take turns analyzing the output. On exciting the output can be fractionated for offline analysis and/or preparative collection.

The reaction studied was a Suzuki-Miyaura reaction and a typical mix consisted of an aryl bromide, a boronic acid, palladium acetate and a phosphine for example triphenylphosphine with a base added and with solvents.