Design And Synthesis Of Fused Pyridine Building Blocks For Automated Library Generation
CHEMMEDCHEM(2021)
Abstract
We demonstrate that a diboration-electrocyclization sequence provides access to a range of pyridine-fused, small-molecule boronic ester building blocks, and that these are amenable to high-throughput synthesis leading to biaryl and ether-linked compound libraries. Moreover, the implementation of an integrated physicochemical and ADME profiling workflow allows accelerated design of novel lead compounds for application in drug-discovery projects.
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Key words
ADME, boron, compound libraries, physicochemistry, pyridines
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