- Palladium Catalyzed Ring Expansion Reaction of Isoxazolones with Isocyanides: Synthesis of 1,3-Oxazin-6-One Derivatives
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A palladium catalyzed ring expansion reaction of isoxazolones with isocyanides was disclosed. In the reaction, a cascade process involving ring-opening/cyclization was suggested. The reaction features high atomic economy due to no elimination of CO2 occurred. Moreover, products obtained demonstrate aggregation-induced emission properties with relatively high solid-state emission efficiencies. (Figure presented.).
- Zhu, Yi-Ming,Zhang, Wan,Li, Hongkun,Xu, Xiao-Ping,Ji, Shun-Jun
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p. 808 - 818
(2020/12/03)
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- PhIO/Et3N ? 3HF-Mediated Formation of Fluorinated 2H-Azirines via Domino Fluorination/Azirination Reaction of Enamines
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A variety of enamine carboxylic esters and enaminones were converted to the biologically interesting fluorinated 2H-azirines through reactions with PhIF2 generated in situ by PhIO and Et3N ? 3HF in 1,2-dichroloethane, which features the hypervalent iodine reagents-mediated introduction of fluorine atom and formation of the 2H-azirine skeleton under metal-free conditions. The domino reaction is postulated to proceed via a PhIF2-mediated oxidative fluorination and a subsequent azirination of the fluorinated enamine intermediates. (Figure presented.).
- Zhang, Yong,Zhao, Xiaoyuan,Zhuang, Chen,Wang, Senlin,Zhang-Negrerie, Daisy,Du, Yunfei
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supporting information
p. 2107 - 2112
(2018/04/19)
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- Synthesis of trifluoromethylated 2H-azirines through Togni reagent-mediated trifluoromethylation followed by PhIO-mediated azirination
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The reaction of enamine compounds with the Togni reagent in the presence of CuI afforded β-trifluoromethylated enamine intermediates, which were converted directly to biologically interesting trifluoromethylated 2H-azirines by an iodosobenzene (PhIO)-mediated intramolecular azirination in a one-pot process.
- Sun, Jiyun,Zhen, Xiaohua,Ge, Huaibin,Zhang, Guangtao,An, Xuechan,Du, Yunfei
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supporting information
p. 1452 - 1458
(2018/07/05)
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- 3-Aryl-4-(2,6-dimethylbenzylidene)isoxazol-5(4H)-ones as Fungicides
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The invention relates to 3-aryl-4-(2,6-dimethylbenzylidene)isoxazol-5(4H)-ones, to agrochemically active salts thereof, to the use thereof and to methods and compositions for controlling phytopathogenic harmful fungi and insects in and/or on plants or in
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Page/Page column 22
(2012/03/27)
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- METHOD FOR PRODUCING PHENYLALKANE-1-OLS
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The present invention relates to a process for preparing phenylalkan-1-ols in three stages, where an ester condensation in the presence of alkali metal or alkaline earth metal alcoholates is carried out in the first stage.
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Page/Page column 4
(2011/06/10)
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- Structure-activity studies of a series of dipyrazolo[3,4-b:3′,4′-d]pyridin-3-ones binding to the immune regulatory protein B7.1
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The interaction of co-stimulatory molecules on T cells with B7 molecules on antigen presenting cells plays an important role in the activation of naive T cells. Consequently, agents that disrupt these interactions should have applications in treatment of transplant rejection as well as autoimmune diseases. To this end, specific small molecule inhibitors of human B7.1 were identified and characterized. Herein, we report the identification of potent small molecule inhibitors of the B7.1-CD28 interaction. In a high-throughput screen we identified several leads that prevented the interaction of B7.1 with CD28 with activities in the nanomolar to low micromolar range. One of these, the dihydrodipyrazolopyridinone 1, was subsequently shown to bind the V-like domain of human B7.1 at equimolar stoichiometry. With this as a starting point, we report here the synthesis and initial in vitro structure-activity relationships of a series of these compounds.
- Green, Neal J.,Xiang, Jason,Chen, Jing,Chen, Lihren,Davies, Audrey M.,Erbe, Dave,Tam, Steve,Tobin, James F.
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p. 2991 - 3013
(2007/10/03)
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- Baccatin derivatives and a process for producing the same
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The object of the invention is to develop baccatin derivatives useful for preparing taxoid compounds such as paclitaxel and a process for the producing the same. The invention provides baccatin derivatives represented by the general formula (I) as well as a process for producing baccatin derivatives represented by the general formula (I) above, which comprises allowing a baccatin represented by the general formula (II) to react with a β-ketoester in the absence of a catalyst or in the presence of a tin compound or an amine base, preferably under reduced pressure.
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