A synthesis of a homologous series of aryl mono- and diboronic acids
Many attempts have been made to prepare aryl boronic acids and their esters which show a preferential affinity for tumor tissues for use in radiation therapy of neoplatic disorders (1,2). The data of Soloway, as extended and refined by Hansch and his coworkers, successfully correlates the low lipid solubility and electron releasing substituents of phyenl boronic acid derivatives with increased tumor concentration (3,4,5). However, most of these organoboron compounds do not produce a sufficiently high tumor-to-normal tissue boron concentration ratio for practical use in human cancer chemotherapy by the neutron capture technique. The knowledge that several chemical substances are preferentially taken up by tumor tissue provides the medicinal chemist the opportunity of rationally designing potential tumor inhibiting compounds linked to these carrier molecules (6,7). For the initial phase of attempts to successfully combine boronic acids or their esters with tumor concentrating material, it was deemed desirable to prepare a homologous series of aryl mono- and diboronic acids
Aromatic compounds Synthesis;Boron compounds, Medicine and Health Sciences, Pharmacy and Pharmaceutical Sciences
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