A new route for the synthesis of tetrahydrocortisone 3-glucuronide has been developed with cortisone acetate as a starting material. The key step was using lithium tri-tert-butoxyaluminum hydride to reduce the C-3 carbonyl group of 5 beta-dihydrocortisone acetate (8) to provide 3 alpha-5 beta-tetrahydrocortisone acetate (5). Then, Koenig-Knorr method was used for glycosylation with glycosyl bromide as the donor, cadmium carbonate as promoter and 4 angstrom molecular sieves as dehydrating agent to give high yield of the desired product. The new route is shorter and gives higher yield than that reported in the literature.