- Preparation method of 1-(4-chlorphenyl)-4, 4-dimethyl-3-pentanone
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The invention discloses a preparation method of 1-(4-chlorphenyl)-4, 4-dimethyl-3-pentanone, and relates to the field of organic chemistry, and the preparation method comprises the following specificsteps: in an autoclave, uniformly mixing a raw material shown as a formula (I) with methanol, wherein a mass ratio of the methanol to the raw material shown as a formula (I) is 2-3: 1; adding a catalyst and a cocatalyst into the mixture; replacing gas in a kettle with mixed gas of nitrogen and hydrogen, introducing hydrogen, performing reacting at the temperature of between 40-100 and 0.1-2.0 MPaunder the hydrogenation pressure, and performing pressure relief, filter pressing, water washing and desolvation to obtain the 1-(4-chlorphenyl)-4, 4-dimethyl-3-pentanone after reaction is performed.The method has the beneficial effects that 1) the reaction yield is 98% or above; and the content is more than 98.5%; 2) the catalyst metallic nickel can be used for more than 20 times; and 3) the content of dechlorinated substances is lower than 0.40%.
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Paragraph 0020-0046
(2020/12/31)
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- Synthesis method of 1-(4-chlorphenyl)-4,4-dimethyl-3-pentanone
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The invention discloses a synthetic method of 1-(4-chlorphenyl)-4,4-dimethyl-3-pentanone. The target compound is prepared through condensation, hydrolysis and decarboxylation, the middle-high pressurehydrogenation step of a traditional process is omitted, and safety is remarkably improved. The method is mild in reaction condition, simple in process and suitable for industrial production.
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Paragraph 0043; 0049-0050; 0054; 0057-0059; 0062-0064; 0067
(2020/08/27)
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- Design, synthesis and neuraminidase inhibitory activity of N-(5-benzyl-4-(tert-butyl)thiazol-2-yl)benzamides
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A series of N-(5-benzyl-4-(tert-butyl)thiazol-2-yl)benzamides were synthesized and the structures were characterized by 1H NMR, MS and elemental analyses. The crystal structures of compounds F5 and F16 were determined by single-crystal X-ray diffraction. The neuraminidase inhibitory activities of compounds F1-F32 were evaluated in vitro at the concentration of 40 μg/mL. The results indicated that compounds F8, F26 and F32 exhibited most potent inhibitory activity against NA. Molecular docking was performed by LeDock to further explain the structure-activity relationship of compound F26. The docking modeling showed that compound F26 was in good combination with oseltamivir binding sites of NA and could be a potential NA inhibitor agent.
- Wu, Zhilin,Peng, Junmei,Hu, Aixi,Ye, Jiao,Li, Guoxi
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p. 356 - 368
(2016/01/25)
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- Synthetic method of tebuconazole intermediate
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The invention provides a synthetic method of tebuconazole intermediate and the chemical name of the tebuconazole intermediate is p-chlorophenyl ethyl tert-butyl ketone. By adopting a dehalogenation inhibitor, the occurrence of dechlorination side reaction is greatly reduced, so that the yield of a traditional process is remarkably improved. According to the synthetic method of the invention, the reaction condition is mild, the process is simple, the usage amount of a catalyst is very low, the average yield of a product reaches 97 percent, and the average purity reaches 98 percent; in addition, the unit operation in the catalytic hydrogenation method provided by the invention is simple and convenient, the production cost is low, and the synthetic method is suitable for the industrial production.
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Paragraph 0044; 0045
(2016/10/07)
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- Process for the hydrogenation of α,β-unsaturated ketones
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The catalytic hydrogenation of α,β-unsaturated ketones of the formula in which R1 and R2 independently of one another represent straight-chain or branched alkyl, hydroxy-alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl or aryl, where at least one of the radicals R1 and R2 is monosubstituted to trisubstituted by halogen, can be carried out on a Ni-containing catalyst and in the presence of an organic sulphur compound of the formula in which R3 and R4 independently of one another denote straight-chain or branched alkyl, hydroxy-alkyl, carboxyalkyl or phenyl, and furthermore R3 and R4 may together represent --CH=CH--CH=CH--, --(CH2)4 --, --(CH2)5 --, --(CH2)2 --S--(CH2)2 -- or --(CH2)2 --O--(CH2)2 --, R4 may additionally denote hydrogen or CO--C1 -C12 -alkyl and n assumes the value 0 or 1.
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- Fungicidal compounds
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Triazoles of formula: STR1 wherein R1 is alkenyl, alkynyl or optionally substituted aralkyl; Y is =N--, R2 is cycloalkyl, alkyl or haloalkyl, and R3 is H, methyl or alkenyl, or esters, ethers, salts and metal complexes thereof. The triazoles have fungicidal and plant growth regulating activity.
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