5750-76-5Relevant academic research and scientific papers
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 for 2,4-dichloropyrimidine and derivatives thereof
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Paragraph 0048; 0049, (2019/04/14)
The invention discloses a preparation method for 2,4-dichloropyrimidine and derivatives thereof. A catalyst, a compound 1 and phosgene are involved in the preparation method. The compound 1 reacts with the phosgene under the action of the catalyst in a solvent. The preparation method is reasonably designed, is convenient for use and is capable of solving the problems of high discharge of phosphorus wastewater and environmental pollution of the traditional process; the end product prepared according to the method is high in conversion rate, the preparation period is short and the problem of environmental pollution is reduced; the method is energy-saving and environment-friendly and is suitable for extensive promotion.
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)
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.
Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV
Zhang, Zhiyuan,Wallace, Michael B.,Feng, Jun,Stafford, Jeffrey A.,Skene, Robert J.,Shi, Lihong,Lee, Bumsup,Aertgeerts, Kathleen,Jennings, Andy,Xu, Rongda,Kassel, Daniel B.,Kaldor, Stephen W.,Navre, Marc,Webb, David R.,Gwaltney, Stephen L.
scheme or table, p. 510 - 524 (2011/03/20)
The discovery of two classes of heterocyclic dipeptidyl peptidase IV (DPP-4) inhibitors, pyrimidinones and pyrimidinediones, is described. After a single oral dose, these potent, selective, and noncovalent inhibitors provide sustained reduction of plasma DPP-4 activity and lowering of blood glucose in animal models of diabetes. Compounds 13a, 27b, and 27j were selected for development.
BENZOTRIAZOLE KINASE MODULATORS
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Page/Page column 45, (2008/06/13)
The invention is concerned with novel benzotriazole derivatives of Formula (I) Wherein R, R1, R2, R3, and m are as defined in the description and the claims, as well as physiologically acceptable salts thereof. These compounds are JNK and CDK modulators.
PYRIMIDINE KINASE INHIBITORS
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Page/Page column 39-42, (2008/06/13)
The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula (I) wherein ring A, X, Y, Z, R1, R2, R3, R4, m and n are as defined herein.
Pyrimidine derivatives useful as inhibitors of PKC-theta
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Page/Page column 108, (2008/06/13)
Disclosed are novel compounds of formula (I): wherein X, Y, R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
