1200341-42-9Relevant academic research and scientific papers
Conception and evolution of stereocontrolled strategies toward functionalized 8-aryloctanoic acids related to the total synthesis of aliskiren
Hanessian, Stephen,Chnard, Etienne,Guesn, Sbastien,Cusson, Jean-Philippe
, p. 9531 - 9545 (2015/02/19)
A detailed account is given describing the approaches used toward the total synthesis of aliskiren. In particular, ring-closing metathesis with the Hoveyda-Grubbs catalyst accelerates the formation of a 9-membered lactone from an (R)-ester. The diastereom
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.
