High-throughput Synthetic Chemistry Enabled By Organic Solvent Disintegrating Tablet

Synthetic chemistry is still a time and labor intensive process with inherent hazardous nature.There are many problems in common practice of synthetic chemistry:1)time and labor consuming by weighing each compound;2)high chance of contact with poisonous chemicals;3)inherent safety hazards in handling of reactive reagents（e.g.Li Al H₄）;4)spoil of reagents chemical is wasteful;and it is often difficult to determine whether a reagent is in good condition;5)low efficacy/high cost caused by using of a glovebox;6)inaccurate dosage of small amount of reagents/catalysts.In order to solve these problems,a new concept of organic solvent disintegrating tablet（O-Tab）was introduced.Organic solvent disintegrating tablet（O-Tab）technology could transform the common practice of synthetic chemistry.Like pharmaceutical tablets,our reagents containing O-Tab is mechanically strong,but disintegrates rapidly when in contact with reaction media（organic solvents）.For O-Tab containing sensitive chemicals,it can be furthered coated to insulate it from air and moisture.Based on the technology of modern drug tablet preparation,we selected the appropriate binder,filler,disintegrant and glidant,which were mixed with the target chemical reagents,and prepared the organic solvent disintegrating tablet by dry compaction.The quality of O-Tabs were then be evaluated.And these organic solvent disintegration tablets were applied to the typical chemical reactions.It proved that the excipients were inert and insoluble.In addition,several components（reagents,catalysts,ligands and additives）were mixed to produce an organic solvent disintegrating tablet（Combo O-Tab）of mixed reagents,which was not only convenient,but also reduced the chance of contact with toxic chemicals,and made it more safe for highly reactive chemicals.Finally,the organic solvent disintegrating tablet containing trace reagent was applied to the high-throughput chemical reactions to screen the reaction condition quickly and effectively reduced the cost of the precious chemicals.