- Process for synthesis of cytosine
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The invention discloses a process for synthesizing cytosine. A 3-hydroxyacrylonitrile compound and an O-methylisourea compound or an S-methylisothiourea compound or an S-ethylisothiourea compound or an S-benzylisothiourea compound are used as raw materials. The process comprises the steps of adding a catalyst and an organic solvent into a reaction kettle, stirring, and then adding the raw materials; heating the mixture to be 50-90 DEG C, and reacting for 8-12 hours; evaporating the solvent to obtain an intermediate; adding concentrated hydrochloric acid into the intermediate, heating to be 70-100 DEG C, and preserving the heat for 1-2 hours; adding water, performing hot filtration, and cooling the obtained filtrate to room temperature; dripping a sodium hydroxide solution into the filtrate to adjust the pH value to be 7-7.5, and cooling to 10-15 DEG C; filtering after cooling, washing, and drying to obtain the cytosine. The process has the advantages that the process steps are simple, the production period is short, and the cost is low; the conversion rate of the raw materials is high, and the synthesized product is good in quality and high in yield, so that the process is suitable for industrialized production.
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Paragraph 0010; 0017
(2017/05/05)
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- Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors
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A high throughput screening (HTS) hit, 1 (Plk1 Ki = 2.2 μM) was optimized and evaluated for the enzymatic inhibition of Plk-1 kinase. Molecular modeling suggested the importance of adding a hydrophobic aromatic amine side chain in order to improve the potency by a classic kinase H-donor-acceptor binding mode. Extensive SAR studies led to the discovery of 49 (Plk1 Ki = 5 nM; EC50 = 1.05 μM), which demonstrated moderate efficacy at 100 mpk in a MiaPaCa tumor model, with no overt toxicity.
- Zhang, Qingwei,Xia, Zhiren,Mitten, Michael J.,Lasko, Loren M.,Klinghofer, Vered,Bouska, Jennifer,Johnson, Eric F.,Penning, Thomas D.,Luo, Yan,Giranda, Vincent L.,Shoemaker, Alexander R.,Stewart, Kent D.,Djuric, Stevan W.,Vasudevan, Anil
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supporting information
p. 7615 - 7622
(2013/02/23)
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- INHIBITORS OF POLO-LIKE KINASES
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Compounds that inhibit Plk1, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.
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Page/Page column 50
(2008/06/13)
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- Antibacterial compounds
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Bacterial protein synthesis-inhibiting compounds having formula (I) and salts, prodrugs, and salts of prodrugs thereof, processes for making the compounds and intermediates in the processes, compositions containing the compounds, and methods of using the compounds are disclosed.
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Page/Page column 19
(2010/02/12)
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- Novel cephalosporin compounds and processes for the preparation thereof
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The present invention relates to novel cephalosporin compounds, pharmaceutically acceptable non-toxic salts, physiologically hydrolyzable esters, hydrates and solvates and isomers thereof which possess potent and broad antibacterial activities. The compounds of the present invention have a (1,5,6-substituted-4-aminopyrimidinium-2-yl)thiomethyl group in 3-position of the cephem nucleus and is specifically represented by the following formula(I): ψψψ
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