4755-77-5Relevant articles and documents
A continuous flow synthesis of [1.1.1]propellane and bicyclo[1.1.1]pentane derivatives
Donnelly, Kian,Baumann, Marcus
supporting information, p. 2871 - 2874 (2021/03/23)
A continuous flow process to generate [1.1.1]propellane on demand is presented rendering solutions of [1.1.1]propellane that can directly be derivatised into various bicyclo[1.1.1]pentane (BCP) species. This was realised in throughputs up to 8.5 mmol h-1providing an attractive and straightforward access to gram quantities of selected BCP building blocks. Lastly, a continuous photochemical transformation of [1.1.1]propellane into valuable BCPs bearing mixed ester/acyl chloride moieties was developed.
Synthesis and application of oxalic acid monoester derivatives
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Paragraph 0015-0018, (2020/12/08)
The invention relates to synthesis and application of oxalic acid monoester-containing compounds as shown in a general formula (I) which is described in the specification. The compounds represent a broad-spectrum efficient insecticidal and bactericidal agent structure type. The oxalic acid monoester-containing compounds can well control aphids, plutella xylostella and spodoptera exigua when used as novel insecticidal bactericides; the compounds can also be used for preventing and treating cucumber brown blotch, cucumber bacterial angular leaf spot, cucumber fusarium wilt, cucumber downy mildew, cucumber powdery mildew, tomato bacterial leaf spot and rice sheath blight. R in the general formula (I) is as defined in the specification.
An ultraviolet absorbent preparation method (by machine translation)
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Paragraph 0043-0047; 0054-0058, (2019/10/29)
The invention relates to an ultraviolet-absorbing agent preparation method, comprises the following steps: (1) D. amide esters intermediate synthesis: to oxalyl chloride ethyl ester and O-ethyl aniline as the raw material, the oxalyl chloride ethyl ester dissolved in a solvent, heating the stirring, then instillment neighbour ethyl aniline, after the reaction water elution solvent, to obtain D. amide esters intermediate; (2) N - (2 - ethoxy) - N' - (4 - ethyl-phenyl) - ethylenediamine amide product synthesis: in order to O-phenetidine and steps (1) obtained in the D. amide esters intermediate as raw materials, to Lewis base as catalyst, the temperature of the stirring, the reaction after 120 - 170 °C lower, boil off ethanol byproducts, cooling, is poured into the methanol stirring and dissolving, filtering out the insoluble matter, the temperature crystallization mother liquor, filtration, and dried to obtain the product. The preparation method, the process is simple, low requirements on equipment; the product has high purity, high yield, three wastes, environmental protection, low production cost, is suitable for industrial production. (by machine translation)
Silver-Catalyzed Cyclization of Propargylic Amides to Oxazolines
Wong, Valerie H. L.,White, Andrew J. P.,Hor,Hii
supporting information, p. 3943 - 3948 (2016/01/25)
A ligand-accelerated effect is observed in the cyclization of propargylic amides catalyzed by bis(pyridyl)silver(I) complexes, with an unexpected reversal of electronic demand to the analogous NH addition reaction. The catalyst was found to be effective for internal alkyne substrates, offering exclusive selectivity for the 5-exo-dig product. Differences in selectivity profile between gold- and silver-catalyzed processes are highlighted and discussed.
METABOTROPIC GLUTAMATE RECEPTORS 5 MODULATORS AND METHODS OF USE THEREOF
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Page/Page column 93, (2012/12/13)
Compounds that modulate GluR5 activity and methods of using the same are disclosed.
Synthesis of 2-aminofurans and 2-unsubstituted furans via carbenoid-mediated [3 + 2] cycloaddition
Jiang, Yaojia,Khong, Vanessa Zhong Yue,Lourdusamy, Emmanuvel,Park, Cheol-Min
experimental part, p. 3133 - 3135 (2012/05/04)
An efficient dual synthetic manifold for 2-aminofurans and 2-unsubstituted furans has been developed. The carbenoid-mediated [3 + 2] cycloaddition of copper carbenoids with enamines provides 2-amino-2,3-dihydrofurans which serve as common intermediates for both 2-aminofurans and 2-unsubstituted furans. The Royal Society of Chemistry 2012.
Design, synthesis and preliminary bioactivity studies of 1,3,4-thiadiazole hydroxamic acid derivatives as novel histone deacetylase inhibitors
Guan, Peng,Sun, Feng'E,Hou, Xuben,Wang, Feng,Yi, Fan,Xu, Wenfang,Fang, Hao
experimental part, p. 3865 - 3872 (2012/08/27)
Histone deacetylase (HDAC) inhibitors have emerged as a new class of anticancer agents, targeting the biological processes including cell cycle, apoptosis and differentiation. In the present study, a series of 1,3,4-thiadiazole based hydroxamic acids were developed as potent HDAC inhibitors. Some of them showed good inhibitory activity in HDAC enzyme assay and potent growth inhibition in some tumor cell lines. Among them, compound 6i (IC50 = 0.089 μM), exhibited better inhibitory effect compared with SAHA (IC50 = 0.15 μM).
Synthesis and evaluation of novel monosubstituted sulfonylurea derivatives as antituberculosis agents
Pan, Li,Jiang, Ying,Liu, Zhen,Liu, Xing-Hai,Liu, Zhuo,Wang, Gang,Li, Zheng-Ming,Wang, Di
scheme or table, p. 18 - 26 (2012/07/01)
A series of novel monosubstituted sulfonylurea derivatives 10a-y were synthesized and characterized by 1H NMR, 13C NMR and HRMS. These compounds were evaluated against Mycobacterium tuberculosis H37Rv in vitro. The results showed compounds 10f, 10k and 10s exhibited moderate antituberculosis activities with MIC values in the range of 20-100 mg/L. Compounds 10b and 10o displayed good antituberculosis activities (MIC 10 mg/L), which were comparable with that of the sulfometuron methyl. Both of the two compounds showed little cytotoxicities, with an IC50 against THP-1 cells greater than 100 mg/L.
Synthesis and cytotoxicity of novel 2-amino-5-thiazolecarboxamide derivatives
Li, Hu,Yue, Yun,Hu, Xiao-Jun,Zhao, Sheng-Yin
scheme or table, p. 416 - 419 (2011/10/08)
A series of novel 2-amino-5-thiazolecarboxamide derivatives have been designed and synthesised. All the compounds were evaluated for their antiproliferative activity against human leukaemia cancer HL 60 and K562 cell lines by standard MTT assay in vitro. Some of these compounds showed moderate cytotoxic potencies. Structure-activity relationships suggested that the piperazine moiety in the side chain of 2-amino-5-thiazolecarboxamide was associated with an increase in the cytotoxicity.
Stereoselective control in the Staudinger reactions involving monosubstituted ketenes with electron acceptor substituents: Experimental investigation and theoretical rationalization
Qi, Hengzhen,Li, Xinyao,Xu, Jiaxi
supporting information; experimental part, p. 2702 - 2714 (2011/05/19)
The stereoselectivity of the Staudinger reactions involving monosubstituted ketenes with electron acceptor substituents was investigated experimentally by determination of the product stereochemistry and theoretically via DFT calculations. The results indicate that imines preferentially attack the less sterically hindered exo-side of the ketenes to generate zwitterionic intermediates. Subsequently, for cyclic imines, the intermediates undergo a conrotatory ring closure directly to produce β-lactams, while for linear imines, the imine moiety of the intermediates isomerizes to more stable intermediates, which further undergo a conrotatory ring closure to afford trans-β-lactams. The steric hindrance and the isomerization, rather than the torquoelectronic effect, play crucial roles in controlling the stereoselectivity in the practical Staudinger reactions involving monosubstituted ketenes with electron acceptor substituents, although the unaccessible borylketene with a powerful electron acceptor group controls the stereoselectivity torquoelectronically, in theory.
