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.
Enantioselective biomimetic transamination of α-keto acids catalyzed by H4-naphthalene-derived axially chiral biaryl pyridoxamines
Hou, Chengkang,Zhao, Guoqing,Xu, Dongfang,Zhao, Baoguo
supporting information, p. 1028 - 1033 (2018/02/15)
Asymmetric biomimetic transamination is a highly attractive method for synthesis of chemically and biologically important chiral amino acids and chiral amines. Development of chiral pyridoxamines/pyridoxals is the key for the reaction. New axially chiral biaryl pyridoxamines based on H4-naphathene skeleton have been developed. The pyridoxamines display good enantioselectivity and high catalytic activity in asymmetric biomimetic transamination of α-keto acids, affording various optically active unnatural amino acids in 61–98% yields with up to 91% ee's.
A naphthoquine salt preparation process
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Paragraph 0057; 0066-0068, (2018/03/25)
The invention discloses a novel preparation process for naphthoquine salt. The process comprises the four process steps: (1) carrying out catalytic reduction on 1-naphthol; (2) carrying out a reaction on 5,6,7,8-tetrahydro-1-naphthol and diazonium salt of p-aminobenzene sulfonic acid, carrying out reduction to form a hydrochloride solution in diluted hydrochloric acid, and carrying out reflux reaction and ammonia alkalinization; (3) adding formaldehyde and tert-butyl amine for reflux and carrying out cooling and crystallization; and (4) stirring the mixture for reflux, carrying out cooling and crystallization, and washing the obtained solid by ethanol, and drying the solid to constant weight so as to obtain a target compound, wherein the purity is greater than 99% or even 99.5% or more. The requirements can be met without further recrystallization. Compared to a conventional process, in the novel process, the step of drying 5,6,7,8-tetrahydro-1-naphthol and the step of forming solid hydrochloride by 4-amino-5,6,7,8-tetrahydro-naphthol are cancelled, so that the process is simpler, pollution and corrosion of equipment are avoided to the maximum extent, and the product is high in product and the total yield is improved by over 30%.
