Simple, High-Yield Synthesis of Polyhedral Carborane Amino Acids

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J. Am. Chem. Soc. 1996, 118, 1223-1224

Simple, High-Yield Synthesis of Polyhedral Carborane Amino Acids

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Scheme 1a

Stephen B. Kahl* and Ramesh A. Kasar Department of Pharmaceutical Chemistry UniVersity of California, San Francisco 513 Parnassus AVenue San Francisco, California 94143-0446 ReceiVed October 11, 1995 Boron neutron capture therapy (BNCT) is a form of binary cancer therapy that offers the potential of delivering spatially selective, high linear energy transfer radiation to the target cells while sparing surrounding normal tissue.1 BNCT is based on the nuclear reaction that occurs when the stable isotope 10B absorbs a thermal neutron to yield an R particle and a recoil 7Li nucleus. These highly energetic particles have mean free paths of 9 and 5 µm, respectively, resulting in confinement of their kinetic energies to approximately one cell diameter. The neutrons used for activation of this process are of subionizing energy (