4.3 Article Proceedings Paper

Fluorine substituent effects (on bioactivity)

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JOURNAL OF FLUORINE CHEMISTRY
卷 109, 期 1, 页码 3-11

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ELSEVIER SCIENCE SA
DOI: 10.1016/S0022-1139(01)00375-X

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fluorocarbon volatility; lipophilicity; solubility; acidity and basicity; fluorine steric effects

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The characteristic effects of fluorine and fluoroalkyl substituents on the physico-chemical properties of molecules that are important to biological activity of fluorinated compounds are highlighted. The influence of fluorination on acidity, hydrogen-bonding, and lipophilicity that affect compound absorption and distribution is described. The current perspectives on fluorine steric interactions and the controversial role of hydrogen-bonding involving the C-F bond are discussed. (C) 2001 Elsevier Science B.V. All rights reserved.

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