866030-34-4Relevant articles and documents
SYTHESIS OF RENIN INHIBITORS INVOLVING A CYCLOADDITION REACTION
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Page/Page column 59, (2010/11/26)
The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula (III), wherein R, R1, and R' are as defined in the specification, or a salt thereof, and a compound of formula (IV) wherein R, R1, R2 and R' are as defined in the specification, and processes of manufacturing these.
Practical synthesis of an orally active renin inhibitor aliskiren
Dong, Hua,Zhang, Zhi-Liu,Huang, Jia-Hui,Ma, Rujian,Chen, Shu-Hui,Li, Ge
, p. 6337 - 6340 (2007/10/03)
A convergent synthesis of aliskiren was accomplished via the use of Segment AB as the key intermediate, which was prepared via the coupling of the Grignard reagent derived from Segment B with Segment A, followed by subsequent oxidative lactonization.