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Increased lipophilicity has been strongly linked with poorer ADME properties and an increased risk of problems with selectivity and toxicology
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Increased lipophilicity has been strongly linked with poorer ADME properties and an increased risk of problems with selectivity and toxicology. Hughes J.D., Blagg J., Price D.A., Bailey S., DeCrescenzo G.A., Devraj R.V., Ellsworth E., Fobian Y.M., Gibbs M.E., Gilles R.W., Greene N., Huang E., Krieger-Burke T., Loesel J., Wager T., Whiteley L., and Zhang Y. Bioorg. Med. Chem. Lett. 18 (2008) 4872
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33847805890
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Compound 16 was synthesised by the same method as used for methyl 3-oxo-5-phenylpentanoate, using 3-chlorobenzyl bromide instead of benzyl chloride
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Compound 16 was synthesised by the same method as used for methyl 3-oxo-5-phenylpentanoate, using 3-chlorobenzyl bromide instead of benzyl chloride,. Huckin S.N., and Weiler L. J. Am. Chem. Soc. 96 (1974) 1082
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The required amidines were either commercially available or readily synthesised from the corresponding nitriles using the Pinner reaction
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