2150-38-1Relevant articles and documents
Kopsirachin, ein ungewoehnliches Alkaloid aus der Apocynaceae Kopsia dasyrachis Ridl.
Homberger, Katharina,Hesse, Manfred
, p. 237 - 248 (1984)
From the leaves of Kopsia dasyrachis Ridl, a new typ of alkaloid, kopsirachine (1) built up from catechin (2) and skytanthine (3) has been isoled.The structure elucidation is based on spectral and chemical evidence.Oxidative cleavage of its derivative 4 with KMnO4 afforded veratric acid which was identified as its methylester by comparison with an authentic sample.Pyrolysis of 1 yielded δ-skythanthine (3).The stereochemistry of the skythanthine substrituents in 1 could not yet be estabilished.
Tyrosinase Inhibitor from Black Rice Bran
Miyazawa, Mitsuo,Oshima, Teruo,Koshio, Katsuya,Itsuzaki, Yumi,Anzai, Jun
, p. 6953 - 6956 (2003)
The inhibitor of tyrosinase activity in black rice bran was investigated. The methanol extract from black rice bran was re-extracted with hexane, chloroform, ethyl acetate, or water. The ethyl acetate extract had the most potent inhibition against tyrosinase activity by 80.5% at a concentration of 0. 4 mg/mL. Inhibitory compound in the ethyl acetate fraction was isolated by silica gel column chromatography, and identified as protocatechuic acid methyl ester (compound 1) by GC, GC-MS, IR, and 1H and 13C NMR spectroscopy. Compound 1 inhibited 75.4% of tyrosinase activity at a concentration of 0.50 μmol/mL. ID50 (50% inhibition dose) value of compound 1 was 0.28 μmol/mL. To study the structure-activity relationship, protocatechuic acid (2), vanillic acid (3), vanillic acid methyl ester (4), isovanillic acid (5), isovanillic acid methyl ester (6), veratric acid (7), and veratric acid methyl ester (8) were also assayed.
Br?nsted acid-catalyzed chlorination of aromatic carboxylic acids
Yu, Zhiqun,Yao, Hongmiao,Xu, Qilin,Liu, Jiming,Le, Xingmao,Ren, Minna
supporting information, p. 685 - 689 (2021/04/09)
The chlorination of aromatic carboxylic acids with SOCl2 has been effectively performed by reacting with a Br?nsted acid as the catalyst. Based on this discovery, an efficient catalytic method that is cheaper than traditional catalytic methods was developed. 20 substrates were chlorinated offering excellent yields in a short reaction time. And the SOCl2/Br?nsted acid system has been used in a larger scale preparative reaction. A dual activation mechanism was proposed to prove the irreplaceable system of SOCl2/Br?nsted acid.
BCL-2 INHIBITOR
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Paragraph 0836-0838, (2021/10/22)
Disclosed herein is a compound of Formula (I) for inhibiting both Bcl-2 wild type and mutated Bcl-2, in particular, Bcl-2 G101V and D103Y, and a method of using the compound disclosed herein for treating dysregulated apoptotic diseases.
Palladium-Catalyzed Chlorocarbonylation of Aryl (Pseudo)Halides Through In Situ Generation of Carbon Monoxide
Bismuto, Alessandro,Boehm, Philip,Morandi, Bill,Roediger, Sven
supporting information, p. 17887 - 17896 (2020/08/19)
An efficient palladium-catalyzed chlorocarbonylation of aryl (pseudo)halides that gives access to a wide range of carboxylic acid derivatives has been developed. The use of butyryl chloride as a combined CO and Cl source eludes the need for toxic, gaseous carbon monoxide, thus facilitating the synthesis of high-value products from readily available aryl (pseudo)halides. The combination of palladium(0), Xantphos, and an amine base is essential to promote this broadly applicable catalytic reaction. Overall, this reaction provides access to a great variety of carbonyl-containing products through in situ transformation of the generated aroyl chloride. Combined experimental and computational studies support a reaction mechanism involving in situ generation of CO.