Bioorganic and Medicinal Chemistry of Fluorine by Jean-Pierre Bégué

By Jean-Pierre Bégué

  • presents a radical evaluation of the function of fluorine in pharmaceutical technological know-how and improvement
  • comprises chapters on fluorinated analogues of common items, fluorinated amino acids and peptides, and derivatives of sugars
  • Classifies advertised and in-development fluorinated prescribed drugs in response to their healing sessions
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    The chemistry of fluorinated compounds has undergone a huge and very fast evolution during the last few decades. New easy-to-handle fluorinating and trifluoromethylation reagents have been discovered, and considerable improvements have been accomplished in these fields. Also, the number of building blocks has greatly increased, and the improvements in synthetic methodology are considerable. 1, 2 The synthesis of fluorinated compounds is largely dependent on industry for access to the starting materials (reagents and building blocks).

    11. E. F. Liebman, and A. , VCH Publishers, Deerfield Beach, FL, 1986, Vol. III, Chap. 4. 12. G. A. , ACS Symposium. Series 911, ACS, Washington DC, 2005, p. 156. 13. M. Y. K. Kondratenko, Russian Chem. Rev. 1974, 43, 32. 14. T. Korenaga, K. Kadowaki, T. Ema, and T. Sakai, J. Org. Chem. 2004, 69, 7340. 15. J. A. Jamois, J. Fluorine Chem. 1991, 53, 79. 16. K. Mikami, Y. Itoh, and M. Yamanaka, in Fluorine-Containing Synthons, V. , ACE Symposium Series 911, ACS, Washington DC, 2005, p. 358. 17. A.

    Glyme). However, dissociating media and solvents also enhance the basicity of the fluoride anion, thus favoring the competitive elimination reaction. In order to reinforce the reactivity of fluoride ions, anhydrous metallic fluoride ions (nonsolvated) can be utilized. 2). 8–10 These reagents allow the direct transformation of a C–OH bond (alcohol) to a C–F bond (fluoride). The reaction is effective with primary, secondary, and tertiary alcohols. These reactions are often stereoselective and take place with inversion of the configuration.

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