173334-57-1 Total synthesis of "Aliskiren": The first renin inhibitor in clinical practice for hypertension

We report a "macrocycle route" toward aliskiren, a drug presently marketed for the treatment of hypertension, using a highly stereocontrolled approach starting from a common "isopropyl chiron". Highlights of the synthesis include a challenging RCM reaction to produce a nine-membered unsaturated lactone, a highly stereoselective catalytic Du Bois aziridination, and a regio- and diastereoselective aziridine ring-opening to a vicinal amino alcohol. https://www.lookchem.com/CASDataBase_173334-57-1.htm

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