529-35-1Relevant articles and documents
Anti-AIDS agents 72. Bioisosteres (7-carbon-DCKs) of the potent anti-HIV lead DCK
Wang, Yang,Huang, Shao-Xu,Xia, Peng,Xia, Yi,Yang, Zheng-Yu,Kilgore, Nicole,Morris-Natschke, Susan L.,Lee, Kuo-Hsiung
, p. 4316 - 4319 (2007)
Three 9,10-di-O-(-)-camphanoyl-7,8,9,10-tetrahydro-benzo[h]chromen-2-one (7-carbon-DCK) analogs (3a-c) were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. All three new carbon bioisosteres of the anti-HIV lead DCK showed anti-HIV activity. Compound 3a had an EC50 value of 0.068 μM, which was comparable to that of DCK in the same assay. The preliminary results indicated that 7-carbon-DCK analogs merit attention as potential HIV-1 inhibitors for further development into clinical trials candidates.
Aromatic compound hydrogenation and hydrodeoxygenation method and application thereof
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Paragraph 0094-0095; 0106-0113, (2021/05/29)
The invention belongs to the technical field of medicines, and discloses an aromatic compound hydrogenation and hydrodeoxygenation method under mild conditions and application of the method in hydrogenation and hydrodeoxygenation reactions of the aromatic compounds and related mixtures. Specifically, the method comprises the following steps: contacting the aromatic compound or a mixture containing the aromatic compound with a catalyst and hydrogen with proper pressure in a solvent under a proper temperature condition, and reacting the hydrogen, the solvent and the aromatic compound under the action of the catalyst to obtain a corresponding hydrogenation product or/and a hydrodeoxygenation product without an oxygen-containing substituent group. The invention also discloses specific implementation conditions of the method and an aromatic compound structure type applicable to the method. The hydrogenation and hydrodeoxygenation reaction method used in the invention has the advantages of mild reaction conditions, high hydrodeoxygenation efficiency, wide substrate applicability, convenient post-treatment, and good laboratory and industrial application prospects.
Benzene and fat ring structure of amino acetyl amine compound and use thereof (by machine translation)
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Paragraph 0122; 0123; 0124, (2019/01/06)
The invention relates to a fat ring structure containing benzimidazole amino acetyl amine compound and use thereof. The amino acetamide compounds the amino acetamide compounds, the compounds of the formula I, or its optically active isomer or a pharmaceutically acceptable salt: In formula I, R1 Hydrogen, C1 - C6 Straight or branched chain alkyl or phenyl; R2 For C1 - C7 Straight or branched chain alkyl, 5 - 6 membered of aralkyl, heteroaromatic ring group or cycloalkyl, or substituted 5 - 6 membered aromatic ring radical of, aromatic heterocyclic base or cycloalkyl; A is alkylene or carbonyl; n is 1 - 3 of the integer; wherein the substituted 5 - 6 membered of aralkyl, heteroaromatic ring group or cycloalkyl substituted group is selected from the following groups in one or more than two: halogen, C1 - C3 Alkyl or alkoxy, C1 - C3 Fluorine-containing alkyl group or a fluorine-containing alkyl oxy, nitro or cyano; states fragrance heterocyclic radical of the hetero atom as the nitrogen or sulfur; m is 1 - 3 of the integer. The present invention provides amino acetyl amine compound can be used as antiepileptic drug or ion channel blockers. (by machine translation)
Regioselective and Chemoselective Reduction of Naphthols Using Hydrosilane in Methanol: Synthesis of the 5,6,7,8-Tetrahydronaphthol Core
He, Yuan,Tang, Jinghua,Luo, Meiming,Zeng, Xiaoming
supporting information, p. 4159 - 4163 (2018/07/29)
A regioselective and chemoselective method for catalytic synthesis of biologically interesting 5,6,7,8-tetrahydronaphthols by reduction of naphthols was described. The side aromatic hydrocarbons in naphthols were site-selectively reduced, using hydrosilanes in methanol, allowing for retaining functional phenol scaffolds intact. It presents a rare example of using low-cost and air-stable hydrosilane for catalytic reduction of unactivated aromatic hydrocarbons under mild conditions. This reaction is scalable and proceeds in high selectivity without the formation of 1,2,3,4-tetrahydronaphthol byproducts with toleration of sensitive functionalities such as bromide, chloride, fluoride, ketone, ester, and amide.