- A 4 - chloro - 2, 5 - dimethoxy acetoacetanilide preparation method (by machine translation)
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The invention relates to a 4 - chloro - 2, 5 - dimethoxy acetoacetanilide preparation method, its implementation are as follows: in a reaction container adding organic solvent and 4 - chloro - 2, 5 - two-anisidine, at a temperature of 10 - 100 °C lower, instillment pair ketene, about 0.5 - 5 hours after adding, canada finishes, thermal insulation reaction 0.5 - 4 hours, the reaction is finished, cooled to 0 - 10 °C, discharging the filter press, the crystalline substance is 4 - chloro - 2, 5 - dimethoxy acetoacetanilide, the filtrate is recycled. The method of the invention the resulting product quality is good, high yield, low cost, realizes the zero discharge of waste water or micro-discharge, accord with the green production requirement of environmental protection, the operation is simple, convenient for industrialization. (by machine translation)
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Paragraph 0026; 0027; 0028; 0029; 0030; 0031; 0032-0035
(2017/08/25)
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- Preparation method of 4-Chloro-2,5-dimethoxyacetoace tanilide
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The invention discloses a preparation method of 4-Chloro-2,5-dimethoxyacetoace tanilide. The preparation method particularly comprises the following steps: adding an alcohols solvent or an acetic acid solvent into a reactor, meanwhile, adding 2,5-dimethoxy-4-chloroaniline, controlling the temperature to be 10-100 DEG C, dripping acetyl ketene, and finishing adding after 0.5-4 h, wherein the molar ratio of 2,5-dimethoxy-4-chloroaniline to acetyl ketene is 1:1-1:1.2; and after finish of dripping, preserving the temperature for 0.5-4 h, keeping the material in a fully-dissolved state after finish of reaction, adjusting the pH to be 0.5-5.0, quickly cooling with a refrigerating fluid, quickly stirring, controlling the cooling speed to be 5-40 DEG C/min, enabling 4-Chloro-2,5-dimethoxyacetoace tanilide to be quickly separated out as powder, cooling to -10 DEG C to 20 DEG C, filtering and drying obtain 4-Chloro-2,5-dimethoxyacetoace tanilide. The preparation method is simple, and the enolic isomer content in obtained 4-Chloro-2,5-dimethoxyacetoace tanilide can be controlled to be 50 ppm or below.
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Paragraph 0028; 0029; 0030; 0031; 0032; 0033-0068
(2017/08/28)
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- Preparation technology of novel naphthol AS-IRG (2,5-Dimethoxy-4-chloroacetoacetanilide)
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The invention relates to a preparation technology of novel naphthol AS-IRG (2,5-Dimethoxy-4-chloroacetoacetanilide). The preparation technology is characterized in that a novel separated reaction kettle is firstly designed, a three-blade sweepback axial flow stirrer is arranged in a reaction kettle body, a material inlet is formed in the upper part of the reaction kettle body, a material outlet is formed in the lower part of the reaction kettle body, and the bottom part of the reaction kettle body is provided with a water gathering pipe and a water separating valve; reactions of esterification, hydrolysis, amidation and the like are carried out in the reaction kettle. The preparation technology disclosed by the invention is novel, green and high-yield, water which is produced in a reaction process is effectively separated, amidation reaction equilibrium is promoted to continuously move rightwards, and the product yield of the naphthol AS-IRG is greatly increased through optimizing reaction conditions.
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Paragraph 0021; 0034
(2016/11/17)
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- Discovery and Optimization of Novel, Selective Histone Methyltransferase SET7 Inhibitors by Pharmacophore- and Docking-Based Virtual Screening
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Histone methyltransferases are involved in various biological functions, and these methylation regulating enzymes' abnormal expression or activity has been noted in several human cancers. Within this context, SET domain-containing (lysine methyltransferase) 7 (SET7, also called KMT7, SETD7, SET9) is of increasing significance due to its diverse roles in biological functions and diseases, such as diabetes, cancers, alopecia areata, atherosclerotic vascular disease, HIV, and HCV. In this study, DC-S100, which was discovered by pharmacophore- and docking-based virtual screening, was identified as the hit compound of SET7 inhibitor. Structure-activity relationship (SAR) analysis was performed on analogs of DC-S100 and according to the putative binding mode of DC-S100, structure modifications were made to improve its activity. Of note, compounds DC-S238 and DC-S239, with IC50 values of 4.88 and 4.59 μM, respectively, displayed selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8, and G9a. Taken together, DC-S238 and DC-S239 can serve as leads for further investigation as SET7 inhibitors and the chemical toolkits for functional biology studies of SET7.
- Meng, Fanwang,Cheng, Sufang,Ding, Hong,Liu, Shien,Liu, Yan,Zhu, Kongkai,Chen, Shijie,Lu, Junyan,Xie, Yiqian,Li, Linjuan,Liu, Rongfeng,Shi, Zhe,Zhou, Yu,Liu, Yu-Chih,Zheng, Mingyue,Jiang, Hualiang,Lu, Wencong,Liu, Hong,Luo, Cheng
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p. 8166 - 8181
(2015/11/09)
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- Process for improving the application properties of disazo pigments
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Process for improving the application properties of disazo pigments obtained by coupling bis-diazotized chlorine-substituted 4,4'-diaminobiphenyls with acetoacetylaminobenzenes, which includes adding sulfite ions to the pigment suspension obtained in the coupling and then heating for one half to two hours at 50° to 100° C. The process produces, above all in large scale industrial batches, a product of uniform quality and having acceptable fastness to solvents, overlacquering, migration and bleeding.
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