28924-21-2Relevant articles and documents
Design, synthesis, and properties of nonlinear optical chromophores based on a verbenone bridge with a novel dendritic acceptor
Sun, Hejing,Li, Zhong'An,Wu, Jieyun,Jiang, Zhenhua,Luo, Jingdong,Jen, Alex K.-Y.
, p. 2840 - 2847 (2018)
Two novel second order nonlinear optical (NLO) chromophores based on N,N-diethylaniline as a donor, verbenone based tetraene as a bridge, and tricyanofuran (TCF) or tricyanofuran derivatives with a dendritic moiety as an acceptor have been synthesized in good overall yields and systematically characterized. Besides, a facile applicable synthetic approach for a NLO dendritic acceptor was developed. Compared with C7, after introducing dendritic derivative steric hindrance groups into the acceptor, chromophore C8 had good thermal stabilities with high thermal decomposition temperatures which were 33 °C higher than that of chromophore C7. At the same time, cyclic voltammetry (CV) experiments were performed to determine the different redox properties. The conjugated verbenone tetraene segments in two chromophores could significantly improve the glass-forming ability and molecular polarization of chromophores as revealed by UV-vis-NIR absorption measurements. The bulky dendritic moiety linked by a short C-C bond is closer to the TCF acceptor, which is the most polar part in the chromophore, compared to conventional isolation groups. The results obtained from electro-optic (EO) coefficients indicate that this TCF acceptor with a unique dendritic structure can prevent antiparallel packing between chromophores, improving the poling efficiency and enhancing the EO performance. These properties, together with the good solubility, suggest the potential use of these new chromophores as materials for advanced photonic devices.
Cannabidiol derivative and preparation method thereof
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Paragraph 0149-0154, (2021/06/06)
The invention provides a cannabidiol derivative and a preparation method thereof. According to the cannabidiol derivative provided by the invention, a specific structure as shown in a formula I is formed by improving a benzyl substituent and a side chain on the basis of CBD, so that the anti-inflammatory effect of the cannabidiol derivative can be improved, and the toxicity can be reduced.
Preparation method of terbutaline sulfate (by machine translation)
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Paragraph 0032-0036; 0047-0051, (2020/04/17)
The method adopts,hydroxyacetophenone as the starting material 3,5 - to obtain, di 3,5 -benzyloxyacetophenone, 3,5 - dibenzyloxyacetophenone and then generates, DMSO-benzyloxy 3,5 -phenyl,tert-butylamino 1 - [3,5 - ethanol (by hydrogenation debenzil) and sulfuric acid into a salt to obtain dibenzyloxybenzenethanone aldehyde] - 2 - (and then reductive amination with tertiary butylamine.) reaction conditions under, reaction conditions, are avoided, The method disclosed by the invention is cheap and easy to obtain and avoids the use of high-risk highly-toxic agents, by reductive amination . The method disclosed by the invention is low, reaction conditions . The method disclosed by the invention is cheap and easily available. (by machine translation)
Versatile and Enantioselective Total Synthesis of Naturally Active Gnetulin
Shang, Changhui,Kang, Yulong,Yang, Qingyun,Zhu, Qibin,Yao, Chunsuo
, p. 3768 - 3776 (2019/07/12)
A versatile and efficient enantioselective total synthesis of natural isorhapontigenin dimers (?)-gnetulin, (+)-gnetulin, and (±)-gentulin was proposed. By using this method, we were able to synthesize the dimers from commercial available achiral materials in 13 steps, and achieve a 7%–9% overall yield with >98% enantiomeric excess. The key features of the method include the stereocontrolled enantioselective conjugate reduction of 3-arylindenone catalyzed by methyloxazaborolidine (Me-CBS) and the α-arylation of 3-aryl-1-indanones. Benzylic sulfide was accessed in excellent yield through the InCl3-catalyzed thio-etherification reaction between 2,3-diarylindanol and bezylic thiol. The method is practical and might thus be useful in the enantioselective synthesis of the optical antipodes of natural indane derivatives with or without methoxy groups at aromatic rings. (Figure presented.).
A synthesis method of terbutaline sulfate (by machine translation)
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Paragraph 0040-0043, (2018/10/04)
The invention provides a method for synthesis of terbutaline sulfate, the specific synthetic route is: to 3, 5 - dihydroxy acetophenone as raw materials, after phenmethyl protection, oxidation, esterification, reduction ammoniation, debenzylation, finally with sulfuric acid to form the salt to obtain the terbutaline sulfate. The invention provides a preparation method of the terbutaline sulfate, the beneficial effect that: 1, using dimethyl sulfoxide (DMSO) to replace the two connecting selenium dioxide, avoid the use of high-risk reagent, safety and high efficiency; 2, [...] process, small pollution to the environment; 3, the operation is simple, mild reaction conditions, the step is short, low cost, is more suitable for industrial production. (by machine translation)
UREA COMPOUNDS AND THEIR USE AS FAAH ENZYME INHIBITORS
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Page/Page column 31, (2015/02/25)
There is provided a compound having Formula I:(I) wherein: R1 is aryl which is optionally substituted with one or more groups selected from hydroxyl, halogen and C1-4 alkoxy, or R1 is aryl which is substituted with a second aryl group or an aryloxy group, wherein the second aryl group or the aryloxy group is optionally substituted with one or more groups selected from hydroxyl, halogen and C1-4 alkoxy; R2 is C1-4 alkyl; R3 is selected from hydroxyl and OSO2CH3; R4 and R5 are independently selected from hydrogen, hydroxyl and halogen; and n is 0 or 1; or a pharmaceutically acceptable salt thereof; wherein when R3 is hydroxyl and R4 and R5 are not hydroxyl, the optionally substituted aryl group, second aryl group or aryloxy group of R1 is substituted with one or more hydroxyl groups or C1-4 alkoxy groups, or wherein when R3 is hydroxyl, one of R4 and R5 is hydroxyl, provided that the compound is not N-(1-benzylpiperidin-4-yl)-4-(3,4-dihydroxyphenyl)-N-methyl-1H-imidazole-1-carboxamide hydrobromide. The compound may be used as an inhibitor of fatty acid amide hydrolase.
Design, synthesis and SAR study of hydroxychalcone inhibitors of human β-secretase (BACE1)
Ma, Lei,Yang, Zhengyi,Li, Chenjing,Zhu, Zhiyuan,Shen, Xu,Hu, Lihong
experimental part, p. 643 - 648 (2012/04/10)
According to the structural characteristics of isoliquiritigenin from Glycyrrhiza uralensis, a series of hydroxychalcones has been designed, synthesized and evaluated for their in vitro inhibitory activities of β-secretase (BACE1). Structure-activity relationship study suggested that inhibitory activity against BACE1 was governed to a greater extent by the hydroxyl substituent on A-and B-ring of the chalcone, and the most active compound was substituted with four hydroxyl group (17, IC50=0.27 μM).
The proline-catalyzed asymmetric amination of branched aldehydes
Baumann, Thomas,Vogt, Henning,Braese, Stefan
, p. 266 - 282 (2007/10/03)
An efficient access to configurationally stable α,β- disubstituted α-amino aldehydes, oxazolidinones, and α-amino acids has been presented. Starting from simple and easily available racemic aldehydes, the α-aminated products were obtained using azodicarboxylates as the nitrogen source in up to 86 % ee and moderate to excellent yield. These products could further be converted both into the corresponding α-amino alcohols and, depending on the residue of the azodicarboxylates and the reaction conditions, into the oxazolidinones. On the other hand, oxidation towards the carboxylic acid and cleavage of the hydrazide bond under mild conditions revealed the free α-alkylated phenylglycine derivative. Wiley-VCH Verlag GmbH & Co. KGaA, 2007.
Asymmetric transfer hydrogenation of ketones catalyzed by hydrophobic metal-amido complexes in aqueous micelles and vesicles
Wang, Fei,Liu, Hui,Cun, Linfeng,Zhu, Jin,Deng, Jingen,Jiang, Yaozhong
, p. 9424 - 9429 (2007/10/03)
Asymmetric transfer hydrogenation of ketones, especially α-bromomethyl aromatic ketones, catalyzed by unmodified, hydrophobic transition metal-amido complexes (TsDPEN-M), was performed successfully with significant enhancement of activity, chemoselectivity, and enantio-selectivity (up to 99% ee) in aqueous media containing micelles and vesicles. The hydrophobic catalyst, embedded in micelles constructed from the surfactant cetyltrimethylammonium bromide (CTAB), could be separated from the organic phase along with the products and was recycled for at least six times.
Effects of the neoflavonoid coutareagenin, one of the antidiabetic active substances of Hintonia latiflora, on streptozotocin-induced diabetes mellitus in rats
Korec, Rudolf,Sensch, Karl Heinz,Zoukas, Thomas
, p. 122 - 128 (2007/10/03)
In the present study, diabetes mellitus was induced with streptozotocin in Wistar rats from the inbred strain F > 28, and a blood sugar lowering effect due to the oral or intragastric administration of a copalchi native extract (Hintoniae latiflorae cortex) or intragastric administration of the pure substance, coutareagenin (neoflavonoid) (5-hydroxy-7-methoxy-4-(3,4- dihydroxyphenyl)-2H-benzo-1-pyran-2-on), was demonstrated with statistically significant results. This study enlarged and confirmed the results of earlier studies by other authors with regard to the antidiabetic effect of the copalchi bark extract in various animal species with hyperglycemia induced by different methods. By the use of the synthetically produced neoflavonoid, coutareagenin, the present series of tests provided evidence that coutareagenin, one of the active substances contained in Hintonia latiflora bark (Copalchi bark), produces a reduction of diabetic elevated blood sugar levels. The native extract as a whole, however, has to be regarded as the active substance (active substance complex) of Hintonia latiflora (Copalchi) bark.
