Coupling of Amino Carboranes to Carboxylic Acid Containing Substrates.

The reactivity of the known amino carboranes 1-H(2)NCH(2)-1,2-C(2)B(10)H(11) and 7-H(3)N-7-CB(10)H(12) with carboxylic acid containing substrates was investigated. The reactions studied using the coupling reagent, 1,1'-carbonyldiimidazole, resulted in the preparation of a series of amides in moderate to high yield. The relative importance of this type of research resides in the fact that it allows the introduction of amino acids in close contact with the carborane cage. These compounds can constitute a new generation of substrates useful in boron neutron capture therapy. Our emphasis lies in the development of suitable synthetic schemes allowing the preparation of this type of compound. Experimental details and analytical data supporting the formulation of the prepared compounds are reported.