1780-31-0Relevant academic research and scientific papers
Synthesis method 2 -fluoro -5 -trifluoromethyl pyrimidine
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Paragraph 0039; 0056-0057, (2021/10/20)
The invention relates to the technical field of drug synthesis, and provides a synthesis method of 2 -fluoro -5 -trifluoromethyl pyrimidine. 5 - Methyluracil is used as a raw material and is subjected to cyclic chlorination reaction. Redox reaction, chlorination reaction and fluorination reaction obtain the target product, the process is simple, the raw materials are cheap and easily available, the yield is high, and no heavy metal pollution is generated in the whole process. In the chlorination reaction, phosphorus oxychloride is used for chlorination, chlorine is used for chlorination in the chlorination reaction, the cost of the chlorination reaction is low, phosphorus pentachloride is used for recycling phosphorus oxychloride in the cyclochlorination reaction, and the reaction cost can be further reduced.
Efficient Phosphorus-Free Chlorination of Hydroxy Aza-Arenes and Their Application in One-Pot Pharmaceutical Synthesis
Wang, Jian,Li, Yan-Hui,Pan, Song-Cheng,Li, Ming-Fang,Du, Wenting,Yin, Hong,Li, Jing-Hua
supporting information, p. 146 - 153 (2020/03/10)
The chlorination of hydroxy aza-arenes with bis(trichloromethyl) carbonate (BTC) and SOCl2 has been effectively performed by refluxing with 5 wt % 4-dimethylaminopyridine (DMAP) as a catalyst. Various substrates are chlorinated with high yields. The obtained chlorinated aza-arenes can be used directly with simple workup for succedent one-pot synthesis on a large scale.
Preparation method of chloro-substituted polyhydroxy aza-aromatic ring compound (by machine translation)
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Paragraph 0019; 0020; 0021-0024, (2019/10/01)
The invention discloses a preparation method, namely BTC and SOCl, of a chloropolyhydroxyl aza heteroaromatic ring compound as a raw material with a polyhydroxy aza heteroaromatic ring compound as a raw material, and a preparation method thereof. 2 As the double chlorination reagent, a chloropolyhydroxyl aza-aromatic ring compound is produced by chlorination reaction with 4 - dimethylaminopyridine (DMAP) as a catalyst at room temperature to reflux temperature of the reaction, as a catalyst. BTC TC TC TC2 /DMDMAP chlorination system has high efficiency, high selectivity and chlorine substitution on a polyhydroxy nitrogen heterocyclic compound; the system can replace POCl3 , The production of phosphorus-containing wastewater is avoided. Using BTC as a chlorination reagent, the reaction by-product was HCl and CO. 2 . From the aspects of industrial wastewater treatment, environmental protection and the like, the advantages thereof are obvious; SOCl is distilled off after the reaction is ended. 2 The quantity is almost no loss, can be used repeatedly, and reduces the process cost. (by machine translation)
COMPOUNDS FOR TREATING TUBERCULOSIS
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Paragraph 0099, (2018/09/18)
The present invention relates to pyrimidine compounds and compositions for treating tuberculosis. These compounds may be used to target the F1 domain of F-ATP synthase and may be used with bedaquiline or 6-chloro-2-ethyl-N-[[4-[4- [4-(trifluoromethoxy)phenyl]piperidin-1 -yl]phenyl]methyl]imidazo[1,2-a]pyridine-3-carboxamide (Q203) or a combination thereof.
Large-scale solvent-free chlorination of hydroxy-pyrimidines,-pyridines,- pyrazines and-amides using equimolar POCl3
Wang, Han,Wen, Kun,Wang, Le,Xiang, Ye,Xu, Xiaocheng,Shen, Yongjia,Sun, Zhihua
experimental part, p. 4533 - 4544 (2012/06/30)
Chlorination with equimolar POCl3 can be efficiently achieved not only for hydroxypyrimidines, but also for many other substrates such as 2-hydroxy-pyridines,-quinoxalines, or even-amides. The procedure is solvent-free and involves heating in a sealed reactor at high temperatures using one equivalent of pyridine as base. It is suitable for large scale (multigram) batch preparations.
2,4-DIAMINOPYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF AURORA KINASE
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Page/Page column 44, (2009/06/27)
A 2,4-diaminopyrimidine derivative of the formula (I), or a pharmaceutically acceptable salt thereof, formula (I) wherein R1, R2, R3, R4, X and Y are as defined in the specification; together with processes for their preparation; pharmaceutical compositions containing them; and their use in therapy. The compounds are inhibitors of Aurora kinase.
New compounds
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Page/Page column 16, (2009/07/10)
The present invention encompasses compounds of general formula (1) wherein R1, R2, R4, X, m, n and p are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.
Aryl sulfonamide and sulfonyl compounds as modulators of PPAR and methods of treating metabolic disorders
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Page/Page column 63, (2010/02/14)
Aryl sulfonamide and sulfonyl compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: Identification and optimisation of substituted 2,4-bis anilino pyrimidines
Breault, Gloria A.,Ellston, Rebecca P. A.,Green, Stephen,James, S. Russell,Jewsbury, Philip J.,Midgley, Catherine J.,Pauptit, Richard A.,Minshull, Claire A.,Tucker, Julie A.,Pease, J. Elizabeth
, p. 2961 - 2966 (2007/10/03)
Through chemical modification and X-ray crystallography we identified the 2,4-bis anilino pyrimidines as potent inhibitors of CDK4. Herein, we describe the optimisation of this series.
Synthesis, molecular modeling and biological activity of methyl and thiomethyl substituted pyrimidines as corticotropin releasing hormone type 1 antagonists
McCluskey, Adam,Keller, Paul A.,Morgan, Jody,Garner, James
, p. 3353 - 3361 (2007/10/03)
Four small, targeted libraries of differentially substituted amino pyrimidines were synthesized in moderate to good yields. Excellent regiochemistry was observed for substitution at C2/C4 with selectivity >50 : 1 noted. All analogues were screened for their ability to interact with CRH 1 and CRH2 receptors. In all instances only poor agonistic and/or antagonistic behaviour was noted at CRH2. However, several compounds were potent and selective CRH1 antagonists, most notably 13a K1 = 39 nM. Additionally we have utilized these data and that recently reported by others to refine our original CRH1 pharmacophore (J. Med. Chem., 1999, 42, 2351-2357).
