Synthesis of a Glycosylated ortho‐Carboranyl Amino Acid.

Abstract

The preparation of an ortho-carborane derivative bearing both carbohydrate and amino acid substituents is presented; opening of a glucofuranuro-g-lactone derivative with propargylamines, cycloaddition of decaborane to an acetylenic bond and amidation with a N-Fmoc-glutamate derivative are the key-steps in this synthesis.

Design, Synthesis, and Biological Evaluation of Boron-Containing Macrocyclic Polyamines and Their Zinc(II) Complexes for Boron Neutron Capture Therapy

“…To date, numerous boron-containing analogues including amino acids, biochemical precursors of nucleic acids, carbohydrates, amines, porphyrins, peptides, liposomes, and monoclonal antibodies have been developed . However, most of them do not satisfy the above criteria for clinical applications.…”