Efficient Large-Scale Synthesis of CAT811, a Potent Calpain Inhibitor of Interest in the Treatment of Cataracts

Matthew A. Jones,James M. Coxon,Stephen B. McNabb,Janna M. Mehrtens,Nathan A. Alexander,Seth Jones,Hongyuan Chen,Clémence Buisan,Andrew D. Abell

AUSTRALIAN JOURNAL OF CHEMISTRY（2009）

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摘要

A high-yielding, short, and scalable synthesis of a potent calpain 2 inhibitor (CAT811) is reported. The key step in the sequence involves an intramolecular macrocyclization of a 6-iodonorleucine residue to the side chain of tyrosine.

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关键词

computational chemistry,amino acids,biosensors,enzymes,spectroscopy,photochemistry,organic chemistry,self assembly,mass spectrometry,structure,biocatalysis,reaction mechanisms,density functional theory,surface chemistry,combinatorial chemistry,polymer chemistry,medicinal chemistry,physical chemistry,colloids,sensors,peptide,crystal structures,electrochemistry,nanotechnology,green chemistry,proteins,supramolecular chemistry,ionic liquids,pharmaceutical chemistry,quantum chemistry,biological chemistry,educational,analytical chemistry,macromolecules,ab initio calculations,interfaces,combinatorial,crystallography,kinetics,inorganic chemistry,catalysis

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