Synthesis of New Boron-Rich Building Blocks for Boron Neutron Capture Therapy or Energy-Filtering Transmission Electron Microscopy

✍ Scribed by Stefan Raddatz; Marco Marcello; Hans-Christian Kliem; Helmut Tröster; Michael F. Trendelenburg; Thomas Oeser; Christof Granzow; Manfred Wiessler

• Publisher: John Wiley and Sons
• Year: 2004
• Tongue: English
• Weight: 247 KB
• Volume: 5
• Category: Article
• ISSN: 1439-4227
• DOI: 10.1002/cbic.200300728

✦ Synopsis

Abstract

The synthesis of a new ortho__‐carborane derivative, tetracarboranylketone 4, is reported here. Ketone 4 was prepared from a tetraalkynylated ketone by the addition of decaborane. The keto group was then easily modified to yield the glycosides 17__α and 18β, which contain glucose or galactose, respectively, and the nucleotide 13 b. In addition to ketone 4, which is acyclic, cyclic ketone 8 was also synthesised. X‐ray diffraction analysis of compound 4 indicated the presence of two toluene guest molecules per molecule of the host compound. Furthermore, compound 4 displays a rather low cytotoxicity. These novel products can be used as building blocks to create a new class of biomolecules containing high‐density carborane clusters. Such molecules may constitute powerful tools for applications like Boron Neutron Capture Therapy or Energy‐Filtering Transmission Electron Microscopy.