109744-49-2Relevant articles and documents
A synthetic method of the compound
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Paragraph 0066; 0067; 0073; 0074, (2017/08/25)
The invention relates to the field of chemistry and in particular relates to the field of medical chemistry. The invention aims to find a novel synthetic route suitable for Vb compounds in industrial production and adaptively provides a specific implementation process of the novel synthetic route, so that high-purity low-cost Vb compounds can be obtained. The compound Vb is prepared by taking a compound I as an initial raw material, so that the traditional Vb synthetic process is replaced. With the adoption of the synthetic route disclosed by the invention, the invention has the advantages that 1, dangerous and expensive butyl lithium is not used; 2, hydrogenation is avoided, and expensive metal palladium is avoided; and 3, more important, debenzylation byproducts in the hydrogenation are avoided. Meanwhile, because the price of the compound I is low, after the synthetic route disclosed by the invention is adopted, the industrial production need of the obtained high-purity low-cost compound V can be met.
Engineering of the Conformational Dynamics of Lipase to Increase Enantioselectivity
Yang, Bin,Wang, Hongjiang,Song, Wei,Chen, Xiulai,Liu, Jia,Luo, Qiuling,Liu, Liming
, p. 7593 - 7599 (2017/11/14)
In order to increase the R-enantioselectivity of Candida antarctica lipase B (CALB) toward (R)-3-t-butyl-dimethyl-silyloxy glutaric acid methyl monoester at 30 °C, we engineered CALB conformational dynamics. Based on structural analysis and molecular dynamics simulations, two key residues (D223 and A281) were identified, and three mutants (D223V, A281S, and D223V/A281S) were designed to decrease the conformational dynamics of the pocket and channel. Computational and experimental evaluations were performed for all mutants, with the D223V/A281S mutant exhibiting high R-enantioselectivity (>99.00%; increased from 8.00%) and high space-time yield (107.54 g L-1 d-1 a 5.70-fold increase).
AN IMPROVED PROCESS FOR THE PREPARATION OF AN INTERMEDIATE OF HMG-COA REDUCTASE INHIBITORS
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, (2011/12/02)
The present invention relates to an improved process for the preparation of intermediates of HMG-CoA reductase inhibitors of Formulae-IXa or IXb and further conversion to HMG-CoA reductase inhibitors and pharmaceutically acceptable salts thereof.