Key result
Novel macrocyclic route enables stereocontrolled synthesis of the direct renin inhibitor aliskiren.
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.
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Hanessian et al. (2010) studied this question. Aliskiren synthesis was evaluated. A macrocycle route toward the renin inhibitor aliskiren was developed using a highly stereocontrolled approach starting from a common isopropyl chiron.
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