Abstract: Two boronated methylglucosides,cesium bis(6 deoxy 2,3,4 tri O acetyl α D methyl glucoside) sulfido undecahydro closo dodecaborate(1 ) and tetrabutylammonium 6 deoxy 2,3,4 tri O acetyl α D methylglucosido oxo undecahydro closo dodecaborate(2 ),are synthesized and characterized by IR, 1H NMR and element analysis.After removal of the acetyl groups by basic hydrolysis,their biodistribution is studied with mice bearing hepatoma H22.The results show that they can be concentrated to 10 μg B in 1 g tumor. The boron concentration in blood is relatively low( R (T/B)≈1.8) and can be quickly cleared.