73942-87-7Relevant articles and documents
Design of oxa-spirocyclic PHOX ligands for the asymmetric synthesis of lorcaserin: Via iridium-catalyzed asymmetric hydrogenation
Ye, Xiang-Yu,Liang, Zhi-Qin,Jin, Cong,Lang, Qi-Wei,Chen, Gen-Qiang,Zhang, Xumu
, p. 195 - 198 (2021/01/14)
Phosphine-oxazoline (PHOX) ligands are a very important class of privileged ligands in asymmetric catalysis. A series of highly rigid oxa-spiro phosphine-oxazoline (O-SIPHOX) ligands based on O-SPINOL was synthesized efficiently, and their iridium complexes were synthesized by coordination of the O-SIPHOX ligands to [Ir(cod)Cl]2 in the presence of sodium tetrakis-3,5-bis(trifluoromethyl)phenylborate (NaBArF). The cationic iridium complexes showed high reactivity and excellent enantioselectivity in the asymmetric hydrogenation of 1-methylene-tetrahydro-benzo[d]azepin-2-ones (up to 99% yield and up to 99% ee). A key intermediate of the anti-obesity drug lorcaserin could be efficiently synthesized using this protocol.
PROCESS FOR THE PREPARATION OF BENZAZEPINE-2-ONE DERIVATIVE
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, (2017/09/05)
The present, invention relates to a cost effective, environment friendly industrially viable process for the preparation of 7,8-dimethoxy-1,3-dihydro-2H-3-benzazepine-2-one, an intermediate used in the preparation of ivabradine, without using acid chloride intermediate and condensing agent.
Benzo aza compound, preparation method and use thereof
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Paragraph 0109; 0110, (2017/08/22)
Belonging to the field of pharmaceutical chemistry, the invention relates to a benzoazepine compound, a preparation method and application thereof, in particular to the benzoazepine compound, its preparation method and application in the field of treatment of nervous system diseases, especially application in the field of drug addiction related to dopamine D1 and D3 receptors. The benzoazepine compound and pharmacologically acceptable inorganic or organic salts thereof have a structure shown as formula (I). Results of drug experiments carried out by the invention show that the benzoazepine compound and its pharmacologically acceptable inorganic or organic salts have high antagonistic activity on dopamine D1 and D3, can be used as drug leads for further development of dopamine receptor antagonists with good selectivity and high activity, and can be used as potential drugs for treatment of drug addiction by dopamine D1, D3 receptor antagonists. (formula (I)).
Functional reversal of (?)-Stepholidine analogues by replacement of benzazepine substructure using the ring-expansion strategy
Li, Wei,Zhang, Li,Xu, Lili,Yuan, Congmin,Du, Peng,Chen, Jiaojiao,Zhen, Xuechu,Fu, Wei
, p. 599 - 607 (2016/10/06)
(?)-Stepholidine is an active ingredient of the Chinese herb Stephania and naturally occurring tetrahydroprotoberberine alkaloid with mixed dopamine receptor D1 agonistic and dopamine receptor D2 antagonistic activities. In this work, a series of novel hexahydrobenzo[4,5]azepino [2,1-a]isoquinolines were designed and synthesized as ring-expanded analogues of (?)-Stepholidine. Initial pharmacological assays demonstrated that a benzazepine replacement was associated with significant increase in selectivity and functional reversal at dopamine receptor D1. Compound-(?)-15e (Ki?=?5.32?±?0.01?nm) is more potent than (?)-Stepholidine (Ki?=?13?nm) and was identified as a selective dopamine receptor D1 antagonist (IC50?=?0.14?μm). Moreover, molecular modeling suggested that (?)-15e might exert its dopamine receptor D1 antagonistic activities through interacting with the transmembrane helix 7 of dopamine receptor D1.
PROCESS FOR THE SYNTHESIS OF BENZAZEPINE DERIVATIVES
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Page/Page column 14-15, (2016/06/21)
Process for the synthesis of benzazepine derivatives The invention relates to a process for the synthesis of 7,8-dimethoxy-1,3-dihydro- benzazepin-2-one of formula (II), as well as to a process for the synthesis of compound of formula (I).
PROCESS FOR THE SYNTHESIS OF 7,8-DIMETHOXY-1,3-DIHYDRO-2H-3-BENZAZEPIN-2-ONE COMPOUNDS, AND APPLICATION IN THE SYNTHESIS OF IVABRADINE
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, (2014/10/16)
Process for the synthesis of the compound of formula (I): wherein R represents a para-methoxybenzyl (PMB) group or the following group: Application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.
PROCESS FOR PREPARATION OF IVABRADINE
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Page/Page column 17-18, (2010/07/09)
The present invention describes a new process for optical resolution of [N-[[3,4- dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl]-N-methylamine] which is an intermediate in the preparation of ivabradine.
Synthesis and biological activity of some 1,3-dihydro-2H-3-benzazepin-2- ones with a piperazine moiety as bradycardic agents
Liang, Hong-Yu,Zhang, Deng-Qing,Yue, Yun,Shi, Zhe,Zhao, Sheng-Yin
scheme or table, p. 114 - 119 (2010/06/13)
A series of 1,3-dihydro-2H-3-benzazepin-2-ones with a piperazine moiety were designed and synthesized by treating the common intermediate of 1,3-dihydro-7,8-dimethoxy-3-[3-(1-piperazinyl)-propyl]-2H-3-benzazepin-2-ones with a variety of N-aryl-2-chloroacetamides and acyl chlorides. Their structures have been characterized by 1H-NMR, MS, and elemental analysis. The title compounds were evaluated for their bradycardic activity in vitro. Most of the synthesized compounds exhibited some vasorelaxant activity and heart-rate-reducing activity with bradycardic potency.
A new synthetic approach towards isoquinobenzazepinone and isoindolinobenzazepinone using acid-mediated cyclisation and Heck reaction
Phakhodee, Wong,Ploypradith, Poonsakdi,Sahakitpichan, Poolsak,Ruchirawat, Somsak
experimental part, p. 351 - 356 (2009/04/06)
Six-membered ring cyclisation of N-ethylbenzazepinone, prepared from the condensation of benzazepinone with phenethyl iodide under basic conditions, smoothly provided the corresponding product, isoquino[1,2-b][3]benzazepinone, under acid-mediated conditions. On the other hand, the attempted direct five-membered ring cyclisation using the acid-mediated conditions failed to give the 7,5 fused ring isoindolinobenzazepinone from N-benzylbenzazepinone, but the 7,6 fused ring product was instead obtained. However, five-membered ring cyclisation of N-benzylbenzazepinone could be effected efficiently by employing the Heck reaction followed by catalytic hydrogenation to furnish the desired isoindolinobenzazepinone.
HETEROCYCLIC AMIDE COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Page/Page column 87, (2009/03/07)
The present invention related to novel heterocyclic amide compounds of Formula 1: as disclosed herein or a pharmaceutically accept able salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosedare compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease
