4.4 Article

Synthesis of novel pyrazole derivatives incorporating one dicarba-closo-dodecaborane unit

Journal

TETRAHEDRON LETTERS
Volume 53, Issue 35, Pages 4743-4746

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2012.06.113

Keywords

CB1 receptor; Carborane; Pyrazole

Funding

  1. Ministerio de Ciencia e Innovacion [CTQ2009-08810]
  2. Departamento de Industria, Comercio y Turismo of the Basque Government

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Boron clusters, and especially dicarba-closo-dodecaboranes, can be used as hydrophobic pharmacophores in the design of new drugs. In the current letter, analogs of the CB1 receptor inverse agonist Rimonabant incorporating a carborane cage (either ortho- or meta-carborane) have been synthesized in moderate yields and their structure has been elucidated by means of H-1 NMR, C-13 NMR, B-11 NMR, and HPLC-MS. (C) 2012 Elsevier Ltd. All rights reserved.

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