53979-19-4Relevant academic research and scientific papers
Synthetic method of Brazilane hematoxylin natural product Brazilane
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Paragraph 0018; 0022; 0023, (2021/04/07)
The invention relates to a synthetic method of Brazilian hematoxylin natural product Brazilian, which comprises the following steps: carrying out acetic anhydride monoprotection, Mitsunobu reaction and Desmarin oxidation reaction on a diol compound, and c
Synthetic method of brazilin natural product (+)-Brazilin
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Paragraph 0018; 0024, (2021/03/31)
The invention relates to a synthetic method of a brazilin natural product, namely (+)-Brazilin. According to the synthetic method, a compound 3,4-dimethoxybenzyl alcohol as shown in formula 1 is usedas an initial raw material and is subjected to a nucleophilic substitution reaction, a lithium aluminum hydride reduction reaction, a Lipase PS enzyme catalyzed desymmetry reaction and a Mitsunobu reaction a Dess-Martin oxidation reaction, a one-pot-process Prins/Friedel-Crafts cascade reaction under an acidic condition, and the like so as to synthesize the natural product (+)-Brazilin. Accordingto the invention, reagents used in the method are conventional chemical reagents, reaction conditions are mild, operation is easy, a rate is relatively high, reaction byproducts are few, and synthesissteps are greatly reduced, and therefore, synthesis cost is reduced to a large extent.
Total synthesis of (–)-brazilane via a lipase-catalyzed desymmetrisation reaction
Chang, Honghong,Guo, Xiaofeng,Huang, Shuangping,Tu, Qidong,Xu, Dongdong,Xue, Zhiwei,Yang, Xihua
, (2021/05/27)
Herein, we described the asymmetric total synthesis of (–)-brazilane, an optically active natural product. The key steps of this synthetic approach are a lipase-catalyzed desymmetrisation reaction of a prochiral diol using vinyl acetate to prepare a chira
Covalent Inhibition of Bacterial Urease by Bifunctional Catechol-Based Phosphonates and Phosphinates
Pagoni, Aikaterini,Grabowiecka, Agnieszka,Tabor, Wojciech,Mucha, Artur,Vassiliou, Stamatia,Berlicki, ?ukasz
, p. 404 - 416 (2021/01/13)
In this study, a new class of bifunctional inhibitors of bacterial ureases, important molecular targets for antimicrobial therapies, was developed. The structures of the inhibitors consist of a combination of a phosphonate or (2-carboxyethyl)phosphinate functionality with a catechol-based fragment, which are designed for complexation of the catalytic nickel ions and covalent bonding with the thiol group of Cys322, respectively. Compounds with three types of frameworks, including β-3,4-dihydroxyphenyl-, α-3,4-dihydroxybenzyl-, and α-3,4-dihydroxybenzylidene-substituted derivatives, exhibited complex and varying structure-dependent kinetics of inhibition. Among irreversible binders, methyl β-(3,4-dihydroxyphenyl)-β-(2-carboxyethyl)phosphorylpropionate was observed to be a remarkably reactive inhibitor of Sporosarcina pasteurii urease (kinact/KI = 10 420 s-1 M-1). The high potential of this group of compounds was also confirmed in Proteus mirabilis whole-cell-based inhibition assays. Some compounds followed slow-binding and reversible kinetics, e.g., methyl β-(3,4-dihydroxyphenyl)-β-phosphonopropionate, with Ki? = 0.13 μM, and an atypical low dissociation rate (residence time τ = 205 min).
Preparation method of donepezil hydrochloride for treating Alzheimer's disease
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Paragraph 0036; 0038; 0044; 0050; 0055; 0057, (2017/10/05)
The invention discloses a preparation method of donepezil hydrochloride for treating the Alzheimer's disease. The preparation method comprises the following steps: (1) mixing 3,4-dimethoxy benzaldehyde with diethyl malonate, thus preparing a mixture M1 co
Synthesis and anti-HIV activity of dibenzylbutyrolactone lignans
Yang, Li-Ming,Lin, Shwu-Jiuan,Yang, Tsang-Hsiung,Lee, Kuo-Hsiung
, p. 941 - 944 (2007/10/03)
Five optically active dibenzylbutyrolactone lignans were synthesized through a lipase-catalyzed transesterification route and evaluated for their inhibitory activity against HIV-1 replication in acutely infected H9 cells. Compounds 1 and 2 demonstrated anti-HIV replication activity with an EC50 values of 2.2 and 0.16 μg/ml and a therapeutic index values of 9.1 and 5, respectively. Structure-antiviral activity relationships are discussed.
BENZOPHENANTHRIDINES V. INVESTIGATION OF THE RODIONOV-SUVOROV SCHEME. SYNTHESIS OF 3,3-DIETHOXYCARBONYL-2-(3,4-DIMETHOXYPHENYL)-6,7-DIMETHOXY-1-TETRALONE
Kyong, Dao Hung,Sladkov, V. I.,Suvorov, N. N.
, p. 1732 - 1738 (2007/10/02)
Triethyl 1,3-bis(3,4-dimethoxyphenyl)propane-1,2,2-tricarboxylate was synthesized by the alkylation of the lithium enolate of ethyl homoveratrate with α-bromo(3,4-dimethoxybenzyl)malonic ester.It was converted by intramolecular acylation, catalyzed by BF3
