188879-03-0Relevant articles and documents
Nucleophilic Amination of Methoxy Arenes Promoted by a Sodium Hydride/Iodide Composite
Kaga, Atsushi,Hayashi, Hirohito,Hakamata, Hiroyuki,Oi, Miku,Uchiyama, Masanobu,Takita, Ryo,Chiba, Shunsuke
, p. 11807 - 11811 (2017/09/20)
A method for the nucleophilic amination of methoxy arenes was established by using sodium hydride (NaH) in the presence of lithium iodide (LiI). This method offers an efficient route to benzannulated nitrogen heterocycles. Mechanistic studies showed that the reaction proceeds through an unusual concerted nucleophilic aromatic substitution.
RENIN INHIBITORS
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Page/Page column 22, (2009/09/04)
The present invention relates to novel renin inhibitors of general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (1), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
The discovery and preparation of disubstituted novel amino-aryl-piperidine- based renin inhibitors
Cody, Wayne L.,Holsworth, Daniel D.,Powell, Noel A.,Jalaie, Mehran,Zhang, Erli,Wang, Wei,Samas, Brian,Bryant, John,Ostroski, Robert,Ryan, Michael J.,Edmunds, Jeremy J.
, p. 59 - 68 (2007/10/03)
Recently, trans-disubstituted oxo-aryl-piperidines have been identified as small molecule nonpeptide renin inhibitors for the modulation of hypertension. Herein, we report on the discovery and preparation of a new class of novel cis-disubstituted amino-aryl-piperidines as a mixture of enantiomers that are potent in vitro renin inhibitors and also, possess in vivo antihypertensive activity in a double transgenic mouse model.
Piperidine-renin inhibitors compounds with improved physicochemical properties
Gueller, Rolf,Binggeli, Alfred,Breu, Volker,Bur, Daniel,Fischli, Walter,Hirth, Georges,Jenny, Christian,Kansy, Manfred,Montavon, Francois,Mueller, Marcel,Oefner, Christian,Stadler, Heinz,Vieira, Eric,Wilhelm, Maurice,Wostl, Wolfgang,Maerki, Hans Peter
, p. 1403 - 1408 (2007/10/03)
Piperidine renin inhibitors with heterocyclic core modifications or hydrophilic attachments show improved physical properties (lower lipophilicity, improved solubility). Tetrahydroquinoline derivative rac-30 with a molecular weight of 517 and a log D((pH 7.4)) of 1.9 displays potent and long lasting blood pressure lowering effects after oral administration to sodium depleted conscious marmosets.