1200341-46-3

Upstream product

• 1200341-42-9 (1S,3S,4R,7S,9R)-3,7-diisopropyl-4-(4-methoxy-3-(3-methoxypropoxy)-phenyl)-6-oxo-5-oxa-10-aza-bicyclo[7.1.0]decane-10-sulfonic acid 2,2,2-trichloro-ethyl ester 

Downstream Products

• 1219468-79-7 (2R,3S,5S)-2,2,2-trichloroethyl 5-((1S,3S)-3-(3-amino-2,2-dimethyl-3-oxopropylcarbamoyl)-1-hydroxy-4-methylpentyl)-3-isopropyl-2-(4-methoxy-3-(3-methoxypropoxy)phenyl)pyrrolidine-1-sulfonate 
• 916793-75-4 (2R,3S,5S)-3-isopropyl-5-((2S,4S)-4-isopropyl-5-oxo-tetrahydro-furan-2-yl)-3-isopropyl-2-[4-methoxy-3-(3-methoxypropoxy)-phenyl]-pyrrolidine-1-carboxylic acid tert-butyl ester 
• 916793-76-5 (2R,3S,5S)-tert-butyl 5-((1S,3S)-3-(3-amino-2,2-dimethyl-3-oxopropylcarbamoyl)-1-hydroxy-4-methylpentyl)-3-isopropyl-2-(4-methoxy-3-(3-methoxypropoxy)phenyl)pyrrolidine-1-carboxylate 
• 173338-07-3 tert-butyl (3S,5S,6S,8S)-8-(3-amino-2,2-dimethyl-3-oxopropylcarbamoyl)-6-hydroxy-3-(4-methoxy-3-(3-methoxypropoxy)benzyl)-2,9-dimethyldecan-5-ylcarbamate 
• 173399-03-6 aliskiren 

Relevant academic research and scientific papers

Conception and evolution of stereocontrolled strategies toward functionalized 8-aryloctanoic acids related to the total synthesis of aliskiren

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

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.