36155-36-9Relevant academic research and scientific papers
Synthesis of 2,3,4,5-Tetrahydrobenzo[1,4]thiazepines via N-Acyliminium Cyclization
Deng, Shixian,Cheng, Zhenzhuang,Ingalls, Charles,Kontes, Ferenc,Yan, Jiaming,Belvedere, Sandro
, p. 1801 - 1805 (2017/11/24)
We report an efficient and scalable synthesis of 7-methoxy-2,3,4,5-tetrahydrobenzo[1,4]thiazepine, the core structure of biologically active molecules like JTV-519 and S107. This synthetic route, starting with 4-methoxythiophenol and proceeding via acyliminum cyclization, gives the target product in four steps and 68% overall yield and is a substantial improvement over previously published processes. Nine additional examples of tetrahydrobenzo[1,4]thiazepine synthesis via acyliminium ring closure are also presented.
AGENTS FOR TREATING DISORDERS INVOLVING MODULATION OF RYANODINE RECEPTORS
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Paragraph 0131, (2013/11/05)
The present invention relates to 1,4-benzothiazepine derivatives and their use to treat conditions, disorders and diseases associated with ryanodine receptors (RyRs) that regulate calcium channel functioning in cells. The invention also discloses pharmaceutical compositions comprising the compounds and uses thereof to treat diseases and conditions associated with RyRs, in particular cardiac, musculoskeletal and central nervous system (CNS) disorders.
Agents for treating disorders involving modulation of ryanodine receptors
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Paragraph 0107, (2013/11/05)
The present invention relates to 1,4-benzothiazepine derivatives and their use to treat conditions, disorders and diseases associated with ryanodine receptors (RyRs) that regulate calcium channel functioning in cells. The invention also discloses pharmaceutical compositions comprising the compounds and uses thereof to treat diseases and conditions associated with RyRs, in particular cardiac, musculoskeletal and central nervous system (CNS) disorders.
Oligomerization of ethylene using new tridentate iron catalysts bearing α-diimine ligands with pendant S and P donors
Small, Brooke L.,Rios, Ray,Fernandez, Eric R.,Gerlach, Deidra L.,Halfen, Jason A.,Carney, Michael J.
experimental part, p. 6723 - 6731 (2011/03/17)
Stoichiometric Schiff base condensations of sterically bulky primary amines with acenaphthenequinone yield isolable monoimines. In the presence of iron(II) chloride, the remaining ketone reacts with a second primary amine bearing a pendant donor atom to g
Design, synthesis, and pharmacological effects of structurally simple ligands for MT1 and MT2 melatonin receptors
Carocci, Alessia,Catalano, Alessia,Lovece, Angelo,Lentini, Giovanni,Duranti, Andrea,Lucini, Valeria,Pannacci, Marilou,Scaglione, Francesco,Franchini, Carlo
experimental part, p. 6496 - 6511 (2010/10/02)
A series of phenoxyalkyl and phenylthioalkyl amides were prepared as melatoninergic ligands. Modulation of affinity of the newly synthesized compound by applying SARs around the terminal amide moiety, the alkyl chain, and the methoxy group on the aromatic ring provides compounds with nanomolar affinity for both melatonin receptor subtypes. Affinity towards MT1 and MT2 receptors were modulated also exploiting chirality. The investigation of intrinsic activity revealed that all the tested compounds behave as full or partial agonists.
PROCESS FOR PREPARING BENZOTHIAZEPINES FROM GAMMA-AMINOALKYLBENZENES
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Page/Page column 13-14, (2009/09/26)
The invention provides a process for preparing a 2,3,4,5-tetrahydro[1,4]benzothiazepine of formula: by reacting a [2-(acylaminoethyl)thio]arene of formula with an aldehyde or a multimer thereof, and with an acid. The invention also provides for first reac
