Synthesis of a Tyr3-octreotate conjugated closo-carborane [HC2B10H10]:: a potential compound for boron neutron capture therapy

A novel Tyr(3)-octreotate conjugated closo-carborane as a potential compound for boron neutron capture therapy was obtained via Fmoc solid phase peptide synthesis. The boron cluster [C2B10H11] was introduced through the reaction of 6,9-bis(acetonitrile)decaborane and 5-hexynoic acid yielding a new closo-carborane conjugated carboxylic acid which was coupled subsequently with solid phase conjugated Tyr(3)-octreotate. The final boron-containing peptide was purified by preparative reverse phase HPLC and structural identity was proved applying MALDI-TOF mass spectrometry. (C) 2003 Elsevier Ltd. All rights reserved.