Synthesis of [5,6-3H2]CP-88,818 (β-[5,6-3H2]tigogenin cellobioside)

CP-88,818 (β-tigogenin cellobioside) is a novel hypocholesterolemic and anti-atherosclerosis agent which acts by inhibiting the absorption of dietary and biliary cholesterol. While the exact mechanism of this inhibition is unclear, CP-88,818 is believed to block cholesterol absorption without entering the body. In order to prove this hypothesis, radiolabelled CP-88,818 was needed. Herein, we report the stereoselective synthesis of [5,6-3H2]CP-88,818 in four steps from diosgenin acetate. (author)