- Preparation method of 2-chloro-6-methoxybenzothiazole
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The invention discloses a preparation method of 2-chloro-6-methoxybenzothiazole, and belongs to the field of medical intermediates. The method comprises the following steps: dissolving 2-amino-6-methoxybenzothiazole in an organic solvent, adding a hydrochloric acid solution, dropwise adding a sodium nitrite solution, and after completion of the reaction, adding a hydrochloric acid solution containing a catalyst, cooling, and recrystallizing to obtain a target product. The preparation method disclosed by the invention is simple, the raw materials are easy to obtain, the reagents and drugs usedin an operation process are relatively low in toxicity, reaction conditions are mild, the time is short, the yield is high, the cost is low, three wastes are little, and the target product is high incontent and high in purity, and the suitability for industrial production is achieved.
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Paragraph 0028; 0029; 0030
(2019/03/28)
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- A 2 - methoxy -6 - methoxybenzene and thiazole preparation method (by machine translation)
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The invention discloses a 2 - methoxy - 6 - methoxybenzene and thiazole preparation method, which belongs to the field of chemical synthesis, the method the 2 - amino - 6 - methoxybenzene and thiazole dissolved in organic solvent, adding hydrochloric acid solution, dropping sodium nitrite solution, reaction finishes, adding hydrochloric acid solution containing the catalyst, cooling, recrystallized to obtain the intermediate product, the intermediate product add methanol, sodium methoxide, under the protection of nitrogen, heating the reaction, after the reaction, natural cooling to room temperature, filter, be insoluble, water heating, freezing, filtering, vacuum drying to obtain the 2 - methoxy - 6 - methoxybenzene and thiazole. The invention selects the synthetic route of the few steps, the reaction route is short, controllability of the strong, few by-products, high yield, low cost at the same time, less wastes, high content of the target products, high purity, it is suitable for industrial production. (by machine translation)
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Paragraph 0029-0031; 0035-0036
(2019/04/06)
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- TYROSINE KINASE INHIBITOR AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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The present invention relates to a tyrosine kinase inhibitor and a pharmaceutical composition comprising same. The tyrosine kinase inhibitor of the present invention has the structures as shown in the following formula (I) or (II):
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Paragraph 0326; 0327
(2018/03/25)
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- Preparation, antibacterial evaluation and preliminary structure-activity relationship (SAR) study of benzothiazol- and benzoxazol-2-amine derivatives
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In this study, a novel benzothiazol- and benzooxazol-2-amine scaffold with antibacterial activity was designed and synthesized. Preliminary structure-activity relationship analysis displayed that compound 8t with a 5,6-difluorosubstituted benzothiazole was found to be a potent inhibitor of Gram-positive pathogens, and exhibited some potential against drug-resistant bacteria and without cytotoxicity in therapeutic concentrations. In addition, molecular docking studies indicated that Staphylococcus aureus methionyl-tRNA synthetase might be the possible target of these compounds. Taken together, the present study provides an effective entry to the synthesis of a good lead for subsequent optimization and a new small molecule candidate drug for antibacterial therapeutics.
- Ouyang, Liang,Huang, Yuhui,Zhao, Yuwei,He, Gu,Xie, Yongmei,Liu, Jie,He, Jun,Liu, Bo,Wei, Yuquan
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p. 3044 - 3049
(2012/06/04)
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- Synthesis and antibacterial evaluation of a novel series of 2-(1,2-dihydro-3-oxo-3H-pyrazol-2-yl)benzothiazoles
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The 2-(1,2-dihydro-3-oxo-3H-pyrazol-2-yl)benzothiazole scaffold was selected as a central core structure for the discovery of novel antibacterial compounds. A systematic variation of the substituents on the oxo-pyrazole moiety, as well as on the benzo moiety, led to the creation of a small and focused library of benzothiazoles that was subjected to antibacterial screening. In a first round of screening, activity of the compounds against six representative microorganisms was established. For the most potent congeners, MIC values against S. aureus and P. aeruginosa were determined. The structure-activity relationship study clearly revealed that subtle structural variations influence the antibacterial activity to a large extent. The most potent congeners displayed MIC values of 3.30 μM.
- Stella, Alessandro,Segers, Kenneth,De Jonghe, Steven,Vanderhoydonck, Bart,Rozenski, Jef,Anne, Jozef,Herdewijn, Piet
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experimental part
p. 253 - 265
(2011/09/30)
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- CYANOISOQUINOLINE COMPOUNDS AND METHODS OF USE THEREOF
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The present invention relates to cyanoisoquinoline compounds suitable for use in treating hypoxia inducible factor-mediated and/or erythropoietin-associated conditions. The cyanoisoquinoline compounds of the invention have the following structure: Formula (I).
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Page/Page column 89
(2008/06/13)
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- Process for the preparation of luciferin compounds
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The present invention provides a process for the preparation of compounds of the general formula: STR1 in which X is a hydroxyl group and X1 is a hydrogen atom or a hydroxyl group, and especially of luciferin, by the reaction of D-cysteine with 2-cyanomono- or -dihydroxybenzothiazole obtained from 2-chloromono- or -dimethoxybenzothiazole via a demethylation, wherein the demethylation is accomplished by reaction with iodotrimethylsilane or with a mixture of phenyltrimethylsilane and iodine and hydrolysis under mild conditions of the silyl derivative formed.
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