Synthesis of useful fragments in drug discovery: 2-Amino-5-tert-butylpyridine and its oxidised analogues
Bioorganic & Medicinal Chemistry Letters（2011）
Abstract
A novel synthesis of the fragment, 2-amino-5-tert-butylpyridine, has been described, yielding more highly oxidised precursors to the tert-butyl group as intermediates. Compound 2 has been shown to have improved physicochemical properties over 1, when considering drug-like properties.
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Key words
Fragments,Drug discovery,Metabolic clearance,Drug-like properties
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