1 results about "Isostere" patented technology

This invention belongs to the fields of organic chemistry, medicinal chemistry, and pharmacology, specifically relating to the synthesis of lometapeptide bioelectron isosteres and their application in the preparation of therapeutic drugs for lipid-lowering diseases. A method for preparing lometapeptide bioelectron isosteres mainly includes six steps: 1) Using A and B as starting materials, under nickel catalysis and the action of phosphine ligands, a reaction occurs... endo The reaction [2+2] yielded intermediate I; 2) Intermediate I underwent intramolecular cyclization under thioxanthracene-9-one and photocatalysis to yield intermediate II; 3) Intermediate II was oxidized under alkaline potassium permanganate to yield intermediate III; 4) Intermediate III and C reacted under the action of a condensing agent to prepare amide intermediate IV; 5) Intermediate IV was debenzylated under the action of palladium on carbon and a hydrogen source to prepare amine intermediate V; 6) Intermediate V and D under alkaline conditions underwent a substitution reaction to obtain the final product, lometapetine bioelectron isostere VI. This bioelectron isostere can dose-dependently inhibit the secretion of apolipoprotein B in HepG2 cells and exhibits good kinetic solubility. This compound shows promise for development as a therapeutic drug for hypercholesterolemia-related diseases.