Amin-carbamoyl-10B-boran, Darstellung und biologische Eigenschaften / Amine-carbamoyl-dihydro-10B-borane, Preparation, and Biological Properties

Abstract

Abstract The chemical section deals with the synthesis of sodiumcyano-10B-borhydride (3) from 10B-boric acid trimethyl ester (1) via sodium-10B-borhydride (2). By converting 3 with trimethylammonium chloride, trimethylamine-cyano-10B-borane (4) is formed which, via nitrilium tetrafluoroborate 5, is transformed by water to Trimethylamine-carboxy-dihydro-10B-borane (6). Trimethylamine-ethoxycarbonyl-dihydro-10B-borane (8b) and amine-carbamoyl-dihydro-10B-borane (8c) can be synthesized from the imidazolid 8a. In the biological section an orientation to the toxicity and the tumor affinity of the compounds 6, 7, and 8c are described. Further the possibility is shown by achieving a maximal concentration of 10B-boron in the tumor whilst at the same time retaining as low a concentration of 10B-Boron as possible in the surrounding tissue.