55162-34-0Relevant articles and documents
Synthesis of N-Alkyl Anilines from Arenes via Iron-Promoted Aromatic C-H Amination
Falk, Eric,Gasser, Valentina C. M.,Morandi, Bill
supporting information, p. 1422 - 1426 (2021/03/08)
We report both an intermolecular C-H amination of arenes to access N-methylanilines and an intramolecular variant for the synthesis of tetrahydroquinolines. A newly developed, highly electrophilic aminating reagent was key for the direct synthesis of unprotected N-methylanilines from simple arenes. The reactions display a broad functional group tolerance and employ catalytic amounts of a benign iron salt under mild reaction conditions.
Practical synthesis of a renin inhibitor via a diastereoselective dieckmann cyclization
Gauvreau, Danny,Hughes, Greg J.,Lau, Stephen Y. W.,McKay, Daniel J.,O'Shea, Paul D.,Sidler, Rick R.,Yu, Bing,Davies, Ian W.
supporting information; experimental part, p. 5146 - 5149 (2011/02/23)
A scalable synthesis of a potent renin inhibitor (1) is described. The absolute stereochemistry is set via an unprecedented diastereoselective Dieckmann cyclization directed by a remote chiral protecting group. This transformation enables preparation of chiral 1,3-[3.3.1]-diazabicyclononenes by desymmetrization of alkyl-esters, with selectivities ranging from 4 to 17:1.
NOVEL CASE OF RENIN INHIBITORS
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Page/Page column 30-31, (2009/01/20)
The present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups. The disclosed low molecular weight, orally active renin inhibitors are of non-peptide nature and have long duration of action. The compounds can be used in the treatment of cardiovascular events and renal insufficiency.