13811-71-7Relevant articles and documents
Design, synthesis and biological evaluation of novel diazaspiro[4.5]decan-1-one derivatives as potential chitin synthase inhibitors and antifungal agents
Li, Bing,Wang, Kaiyuan,Zhang, Rui,Li, Baihui,Shen, Yangli,Ji, Qinggang
supporting information, (2019/09/07)
A series of 2,8-diazaspiro[4.5]decan-1-one derivatives were designed, synthesized and screened for their inhibition activities against chitin synthase (CHS) and antimicrobial activities in vitro. The biological assays revealed that compounds 4a, 4e, 4h, 4j, 4o, 4q and 4r exhibited moderated to excellent potency against CHS with IC50 values ranging from 0.12 to 0.29 mM. Compounds 4e, 4j with IC50 value of 0.13 mM, 0.12 mM respectively, showed excellent inhibition potency among these compounds, which were similar to that of polyoxin B whose IC50 value was 0.08 mM. Meanwhile, the screening of the antifungal activity showed that compounds 4j and 4r had the same potency of inhibiting the growth of A. fumigatus with MIC value of 0.08 mmol/L. Compound 4d displayed excellent activity against C. albicans (ATCC 90023) with MIC value of 0.04 mmol/L, which was superior to fluconazole (0.104 mmol/L) and polyoxin B (0.129 mmol/L). The result of antibacterial assay showed that these compounds had little potency against those selected bacteria strains including three Gram-positive bacteria and three Gram-negative bacteria. Furthermore, the combination use of 4c-fluconazole, 4i-fluconazole, 4j-fluconazole, and 4o-fluconazole against C. albicans,A. fumigatus and A. flavus showed additive or synergistic effects. These results indicated that the designed compounds serve as potential chitin synthase inhibitors and have selectively antifungal activities.
High-purity manufacturing method of dialkyl tartrate
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Paragraph 0165-0170, (2017/03/24)
The invention provides an efficient method for manufacturing high purity tartaric acid dialkyl esters, including the steps of: reacting fatty alcohol of alkyl with 1-4 carbon atom(s) with tartaric acid without solvents and acid catalysts, and then performing concentration until moisture content becomes below 1.0 weight% to obtain a first esterification reaction liquid; adding fatty alcohol of a same kind into the first esterification reaction liquid to prepare a homogeneous solution, and then adding thionyl chloride for reaction to perform concentration to obtain a second esterification reaction liquid; adding solid shaped bicarbonate into the second esterification reaction liquid for neutralization, and performing solid-liquid separation, concentration and thin-film distillation. According to the method, high purity tartaric acid dialkyl esters with the content of sulfurous acid dialkyl esters below 0.1% and content of tartaric acid monoalkyl esters below 0.1% is obtained.
Practical synthesis of trans-dihydroxybutyrolactols as chiral C4 building blocks and their application to the synthesis of polyhydroxylated alkaloids
Zeng, Jing,Zhang, Qian,Zhang, Hong-Kui,Chen, Anqi
, p. 20298 - 20307 (2013/11/06)
Practical syntheses of trans-dihydroxybutyrolactols 2a, 2b and 2c from inexpensive chiral pool compounds l-ascorbic, d- and l-tartaric acid have been achieved on a multigram-scale. The synthetic applications of these chiral building blocks have been demonstrated in the efficient total or formal synthesis of polyhydroxylated alkaloids (+)-lentiginosine and (-)-deacetylanisomycin in concise routes. The Royal Society of Chemistry 2013.