5747-92-2Relevant articles and documents
Electrochemical Generation of a Nonstabilized Azomethine Ylide: Access to Substituted N-Heterocycles
Kumar, Rakesh,Banerjee, Prabal
, p. 16104 - 16113 (2021/11/18)
Azomethine ylides are fascinating 1,3-dipoles for [3 + 2] cycloaddition reactions toward the construction ofN-heterocycles. Herein, an efficient and environmentally benign electrochemical approach for the generation of a nonstabilized azomethine ylide has been established under metal-free and external oxidant-free conditions. The resulting 1,3-dipole undergoes a [3 + 2] cycloaddition reaction with olefins. This electrosynthetic methodology indulges a straightforward and facile approach for the construction of substituted pyrrolidines.
Photoinduced Nonstabilized Azomethine Ylide Formation for the Preparation of Fluorine Containing Pyrrolidines
Thierry, Thibault,Lebargy, Cyril,Pfund, Emmanuel,Lequeux, Thierry
, p. 5877 - 5885 (2019/05/10)
A mild and reproducible method for the formation of a nonstabilized azomethine ylide was developed by photoinduced reaction catalyzed with eosin Y under green light irradiation. Resulting 1,3-dipole was trapped with fluoroalkenes, fluoroalkylated alkenes,
Photoinduced Nonstabilized Azomethine Ylide Formation for the Preparation of Fluorine Containing Pyrrolidines
Thierry, Thibault,Lebargy, Cyril,Pfund, Emmanuel,Lequeux, Thierry
, (2019/05/08)
A mild and reproducible method for the formation of a nonstabilized azomethine ylide was developed by photoinduced reaction catalyzed with eosin Y under green light irradiation. Resulting 1,3-dipole was trapped with fluoroalkenes, fluoroalkylated alkenes,
Discovery of novel n-substituted prolinamido indazoles as potent rho kinase inhibitors and vasorelaxation agents
Yao, Yangyang,Li, Renze,Liu, Xiaoyu,Yang, Feilong,Yang, Ying,Li, Xiaoyu,Shi, Xiang,Yuan, Tianyi,Fang, Lianhua,Du, Guanhua,Jiao, Xiaozhen,Xie, Ping
, (2017/11/07)
Inhibitors of Rho kinase (ROCK) have potential therapeutic applicability in a wide range of diseases, such as hypertension, stroke, asthma and glaucoma. In a previous article, we described the lead discovery of DL0805, a new ROCK I inhibitor, showing potent inhibitory activity (IC50 6.7 μM). Herein, we present the lead optimization of compound DL0805, resulting in the discovery of 24- and 39-fold more-active analogues 4a (IC50 0.27 μM) and 4b (IC50 0.17 μM), among other active analogues. Moreover, ex-vivo studies demonstrated that 4a and 4b exhibited comparable vasorelaxant activity to the approved drug fasudil in rat aortic rings. The research of a preliminary structure-activity relationship (SAR) indicated that the target compounds containing a β-proline moiety have improved activity against ROCK I relative to analogues bearing an β-proline moiety, and among the series of the derivatives with a β-proline-derived indazole scaffold, the inhibitory activity of the target compounds with a benzyl substituent is superior to those with a benzoyl substituent.
[3+2] Dipolar cycloadditions of an unstabilised azomethine ylide under continuous flow conditions
Grafton, Mark,Mansfield, Andrew C.,Fray, M. Jonathan
scheme or table, p. 1026 - 1029 (2010/04/02)
The [3+2] dipolar cycloaddition reactions of the unstabilised azomethine ylide precursor benzyl(methoxymethyl)(trimethylsilylmethyl)amine with 12 electron-deficient alkenes in the presence of catalytic trifluoroacetic acid are examined under continuous fl
Tris(pentafluorophenyl)borane-catalyzed synthesis of N-benzyl pyrrolidines
Srihari, Pabbaraja,Yaragorla, Srinivasa Rao,Basu, Debjit,Chandrasekhar, Srivari
, p. 2646 - 2648 (2008/02/04)
1,3-Dipolar cycloaddition of in situ generated azomethine ylides to electron deficient olefins catalyzed tris(pentafluorophenyl)borane is described. Georg Thieme Verlag Stuttgart.
QUINOLONE ANTIBACTERIAL AGENTS
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Page/Page column 69, (2010/02/11)
Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications including use as antibacterial agents.
1-(4-PIPERIDINYL) BENZIMIDAZOLONES AS HISTAMINE H3 ANTAGONISTS
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Page 71-72, (2010/02/04)
Disclosed are histamine H3 antagonists of the formula (I) wherein R1 is benzimidazolone derivative, M1 and M2 are optionally substituted carbon or nitrogen, R2 includes optionally substituted aryl or heteroaryl, and the remaining variables are as defined
The convenient synthesis of 3-alkyloxycarbonylpyrrolidine derivatives
Dong, Jingchao,Kou, Binbin,Li, Runtao,Cheng, Tieming
, p. 935 - 939 (2007/10/03)
A series of 3-alkyloxycarbonylpyrrolidine derivatives are readily achieved via 1,3-dipolar cycloaddition of α,β-unsaturated esters with nonstabilized azomethine ylides in the presence of samarium diiodide.
Oxadiazoles useful in the treatment of senile dementia
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, (2008/06/13)
A class of novel oxadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring, and substituted on the other ring carbon atom with a substituent of low lipophilicity; are potent muscarinic agonists, and have good CNS penetrability. The compounds are therefore useful in the treatment of neurological and mental illnesses.
