- Iron-catalyzed bromination of aryl azides by N-bromosuccinimide: Efficient method for the synthesis of brominated aryl azides
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An efficient and mild protocol for bromination of aryl azides with N-bromosuccinimide (NBS) under FeCl3 catalysis in 1,2-dichloroethane was developed. It is proved to be an efficient method for obtaining brominated aryl azides.
- Jin, Hui,Huang, Zhen Dong,Kuang, Chun Xiang,Wang, Xiao Kun
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Read Online
- Cyclic keto-pyridone-linked heteroaromatic ring compound as well as preparation method and application thereof
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The invention belongs to the field of medicinal chemistry, specifically, the invention relates to a cyclic ketone and pyridone hetero-aromatic ring compound as well as a preparation method and an application of the cyclic ketone and pyridone hetero-aromatic ring compound. The structure of the compound is shown as a general formula (I). The compounds or the stereoisomers, racemes, geometric isomers, tautomers, prodrugs, hydrates, solvates or pharmaceutically acceptable salts and pharmaceutical compositions thereof can be used for treating or/and preventing related diseases mediated by the FXIa (Factor XIa for short).
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Paragraph 0091-0092; 0099-0100
(2021/05/12)
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- Furo-pyridone imidazole compound as well as preparation method and application thereof
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The invention belongs to the field of medicinal chemistry. Specifically, the invention relates to a furo-pyridone imidazole compound as well as a preparation method and application thereof. The structure of the compound is shown as a general formula (I). The compounds or the stereoisomers, racemes, geometric isomers, tautomers, prodrugs, hydrates, solvates or pharmaceutically acceptable salts and pharmaceutical compositions thereof can be used for treating or/and preventing related diseases mediated by the FXIa (Factor XIa for short).
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Paragraph 0158-0162
(2021/07/21)
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- Furo-pyridone amide compound as well as preparation method and application thereof
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The invention belongs to the field of medicinal chemistry. The invention relates to a furo-pyridone amide compound as well as a preparation method and application thereof. Specifically, the structure of the compound is shown as a general formula (I) in th
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Paragraph 0172-0177
(2021/07/21)
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- Alkoxy pyridone compound as well as preparation method and application thereof
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The invention belongs to the field of medicinal chemistry, specifically, the invention relates to a series of inhibitors of factor XIa (FXIa for short) with a novel structure as well as a preparationmethod and an application thereof. The structure is shown as the following general formula (I). These compounds or stereoisomers, racemates, geometric isomers, tautomers, prodrugs, hydrates, solvatesor pharmaceutically acceptable salts and pharmaceutical compositions thereof can be used to treat or/and prevent related diseases mediated by factor XIa (FXIa for short).
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Paragraph 0147-0149
(2020/12/15)
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- Making endo-cyclizations favorable again: A conceptually new synthetic approach to benzotriazoles via azide group directed lithiation/cyclization of 2-azidoaryl bromides
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Although benzotriazoles are important and ubiquitous, currently there is only one conceptual approach to their synthesis: bridging the two ortho-amino groups with an electrophilic nitrogen atom. Herein, we disclose a new practical alternative-the endo-cyclization of 2-azidoaryl lithiums obtained in situ from 2-azido-aryl bromides. The scope of the reaction is illustrated using twenty-four examples with a variety of alkyl, alkoxy, perfluoroalkyl, and halogen substituents. We found that the directing effect of the azide group allows selective metal-halogen exchange in aryl azides containing several bromine atoms. Furthermore, (2-bromophenyl)diazomethane undergoes similar cyclization to give an indazole. Thus, cyclizations of aryl lithiums containing an ortho-X = Y = Z group emerge as a new general approach for the synthesis of aromatic heterocycles. DFT computations suggested that the observed endo-selectivity applies to the anionic cyclizations of other functionalities that undergo "1,1-additions" (i.e., azides, diazo compounds, and isonitriles). In contrast, cyclizations with the heteroatomic functionalities that follow the "1,2-addition" pattern (cyanates, thiocyanates, isocyanates, isothiocyanates, and nitriles) prefer the exo-cyclization path. Hence, such reactions expand the current understanding of stereoelectronic factors in anionic cyclizations.
- Ageshina, Alexandra A.,Chesnokov, Gleb A.,Topchiy, Maxim A.,Alabugin, Igor V.,Nechaev, Mikhail S.,Asachenko, Andrey F.
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p. 4523 - 4534
(2019/05/17)
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- SUBSTITUTED OXOPYRIDINE DERIVATIVES
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The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and o edemas, and also ophthalmic disorders.
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Page/Page column 92-93
(2017/02/09)
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- FACTOR XIa INHIBITORS
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The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma Kallikrein.
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Page/Page column 62-63
(2017/05/21)
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- FACTOR XIa INHIBITORS
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The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.
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Page/Page column 38
(2016/05/02)
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