1219468-81-1Relevant articles and documents
Total synthesis of "Aliskiren": The first renin inhibitor in clinical practice for hypertension
Hanessian, Stephen,Guesne, Sebastien,Chenard, Etienne
supporting information; experimental part, p. 1816 - 1819 (2010/09/16)
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.