Cholesterol Absorption Inhibitor Garment Folding Mab (ezetimibe) Derivatives Synthesis

Abstract:The cholesterol absorption inhibitor ezetimibe takes a vital role in the hyperlipcmia and has good opportunities in the market. We designed a4-deuterated derivative of ezetimibe and evaluated its pharmacology activities and pharmacology dynamics in order to find a highly active, highly selective, safe and reliable compound as the cholesterol absorption inhibitor.The compound was synthesized from the deuterated phenol as the starting materials, following by bromination, phenol’s hydroxyl protection, aldehyde transformation from bromide, coupling and final cyclization to afford the four-deuterated (S)-4-(4-(benzyloxy)phenyl)-1-(4-fluorophenyl)azetidin-2-one. At the same time, the derivative of ezetimibe was also synthesized from but-2-yne-1,4-diol following by hydroxyl protection, reduction, coupling, bromization, coupling and deprotection. Both synthetic routes have high overall yield, less steps, cheap raw materials, mild reaction conditions, and easy work-up.