Fluorine in Heterocyclic Chemistry Volume 1: 5-Membered by Valentine Nenajdenko

By Valentine Nenajdenko

This two-volume paintings combines entire info at the chemistry of the fluorinated heterocycles. the cloth has been divided such that the 1st quantity is devoted to five-membered fluorinated heterocycles and macrocycles, whereas the second one quantity combines info hooked up with the chemistry of fluorine containing six-membered heterocycles. either volumes could be of curiosity to man made natural chemists ordinarily, and especially for these colleagues operating within the fields of heterocyclic-compound chemistry, fabrics chemistry, medicinal chemistry, and fluorine chemistry. All details is gifted and categorized basically to be potent resource for vast auditory of chemists. will probably be fascinating for scientists operating within the box of inorganic and coordination chemistry. Fluorinated heterocycles have gotten more and more vital in lots of components together with the pharmaceutical undefined, fabrics technological know-how and agriculture. The presence of fluorine can lead to sizeable sensible alterations within the organic in addition to physicochemical homes of natural compounds. Incorporation of fluorine into drug molecules can enormously have an effect on their physicochemical houses, akin to bond energy, lipophilicity, bioavailability, conformation, electrostatic power, dipole second, pKa and so forth. in addition to pharmacokinetic houses, corresponding to tissue distribution, cost of metabolism and pharmacological homes, reminiscent of pharmacodynamics and toxicology.

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Additional info for Fluorine in Heterocyclic Chemistry Volume 1: 5-Membered Heterocycles and Macrocycles

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E. the site of oxidation, and then block that site with a substituent resistant to metabolism. One way to accomplish this is to replace a labile/susceptible carbon-bound hydrogen with a fluorine atom. This type of substitution infrequently impairs drug-target interactions and is a strategy that has been employed successfully in many contexts [106–110]. One notable example is the discovery of ezetimibe (63) (Fig. 24), a marketed β-lactam derivative that lowers systemic cholesterol levels by blocking intestinal absorption of cholesterol [108, 109].

One way to accomplish this is to replace a labile/susceptible carbon-bound hydrogen with a fluorine atom. This type of substitution infrequently impairs drug-target interactions and is a strategy that has been employed successfully in many contexts [106–110]. One notable example is the discovery of ezetimibe (63) (Fig. 24), a marketed β-lactam derivative that lowers systemic cholesterol levels by blocking intestinal absorption of cholesterol [108, 109]. A key experiment led to the identification of active metabolites of the prototype compound 62 after dosing to rats [108], which in turn led to the discovery that metabolites were more efficiently localized to the putative site of action of the drug than 62 itself.

Heidelberger C, Chaudhuri NK, Danneberg P, Mooren D, Griesbach L, Duschinsky R, Schnitzer RJ, Pleven E, Scheiner J (1957) Fluorinated pyrimidines, a new class of tumourinhibitory compounds. Nature 179:663–666 14. Bégué J-P, Bonnet-Delpon D (2008) Bioorganic and medicinal chemistry of fluorine. Wiley, Hoboken 15. Böhm H-J, Banner D, Bendels S, Kansy M, Kuhn B, Müller K, Obst-Sander U, Stahl M (2004) Fluorine in medicinal chemistry. ChemBioChem 5:637–643 16. Müller K, Faeh C, Diederich F (2007) Fluorine in pharmaceuticals: looking beyond intuition.

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