An efficient solid-phase synthetic method for 2,3,4,5-Tetrahydro-1,4-benzodiazepin-2,5-diones, having amine derivatives on the benzene ring, was developed. This method has been successfully applied to the synthesis of several spatially separated drug-like and information-rich small-molecule libraries composed of 400 compounds using ACT-496 automatic synthesizer and the IRORI radio frequency-encoded split-mix synthesis technology.
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