- Tandem Schiff-Base Formation/Heterocyclization: An Approach to the Synthesis of Fused Pyrazolo-Pyrimidine/Isoxazolo-Pyrimidine Hybrids
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A new synthesis of pyrazolo[4,3-d]pyrimidines and isoxazolo[4,5-d]pyrimidines is described. Key steps in the synthesis involve Stille coupling of 4,6-dichloro-2-phenyl-pyrimidine with tributyl(1-ethoxyvinyl)stannane and tandem Schiff-base formation/heterocyclization of 2,6-di-aryl-5-fluoro-4-acetylpyrimidine with hydrazines or hydroxylamine to give pyrazolo[4,3-d]pyrimidines and isoxazolo[4,5-d]pyrimidines, respectively. The position of the fluoro group in the A-pyrimidine ring is important for the success of heterocylization reaction.
- Sambaiah,Mallesham, Poosa,Shiva Kumar,Bobde, Yamini,Hota, Prasanta Kumar,Yennam, Satyanarayana,Ghosh, Balaram,Behera, Manoranjan
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- Electropolymerization of [2 × 2] grid-type cobalt(II) complex with thiophene substituted dihydrazone ligand
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The grid-type complex [Co4(L1-2H)4] containing dihydrazone ligand decorated with thiophene rings has been prepared. The complex undergoes oxidative electropolymerization onto ITO electrode to form purple thin film. The morphology of
- Napiera?a, Sergiusz,Kubicki, Maciej,Patroniak, Violetta,Wa??sa-Chorab, Monika
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- Rational drug design of 6-substituted 4-anilino-2-phenylpyrimidines for exploration of novel ABCG2 binding site
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In the search for novel, highly potent, and nontoxic adjuvant chemotherapeutics to resolve the major issue of ABC transporter-mediated multidrug resistance (MDR), pyrimidines were discovered as a promising compound class of modern ABCG2 inhibitors. As ABC
- Silbermann, Katja,Li, Jiyang,Namasivayam, Vigneshwaran,Stefan, Sven Marcel,Wiese, Michael
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- Electronic absorption and emission properties of bishydrazone [2?×?2] metallosupramolecular grid-type architectures
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Several ditopic ligands containing two tridentate bishydrazone coordination subunits and their Zn(II) and Cd(II) [2 × 2] grid-type complexes were prepared and their photoluminescent properties studied. A special attention was devoted to the influence of the orientation of the hydrazone group N–N[dbnd]in the core of the ligands and their complexes. Its reversal from [pyridine[dbnd]N–N–pyrimidine] (L1) to [pyridine–N–N[dbnd]pyrimidine] (L2) has a strong impact on the observed absorption and emission behaviour of particular ligands (L1 and L2) as well as of their [2 × 2] grid assemblies. The further lateral functionalization of the ligands led to different emission quantum yields of the resulting grids, while their emission and absorption spectra varied very little. The simplest derivative L1 turned out to have the best performance with, for its Zn(II) complex, relatively high quantum yield 60%.
- Holub, Jan,Santoro, Antonio,Lehn, Jean-Marie
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p. 223 - 231
(2019/06/07)
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- Preparation and application of neutral C-H bond anion recognition receptor
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The invention discloses a novel compound capable of detecting and recognizing chloride ions, particularly relates to preparation and application of a neutral C-H bond anion recognition receptor, and belongs to the technical field of supramolecular chemistry molecular recognition. The structural formula of the receptor compound is as follows (as shown in the description). Through the pyrimidine receptor compound based on a neutral C-H bond, the anion recognition property can be greatly improved, and the pyrimidine receptor compound and the chloride ion can form a stable complex compound in the proportion of the pyrimidine receptor compound to the chloride ions being 1 to 1. The compound is good in selectivity, high in combining capacity and high in sensitivity, can be used for detecting and recognizing the chloride ions in biological samples or environmental samples, and has good application prospects.
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Paragraph 0016
(2017/02/17)
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- 'Green' synthesis of 2-substituted 6-hydroxy-[3H]-pyrimidin-4-ones and 4,6-dichloropyrimidines: Improved strategies and mechanistic study
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An improved route to 2-substituted 6-hydroxy-[3H]-pyrimidin-4-ones 4 and to 2-substituted 4,6-dichloropyrimidines 5 is reported. Without using highly toxic reactants, compounds 4 can be prepared conveniently in a one pot synthesis on a one mol scale with average yields up to 80%. 4,6-Dichloropyrimidines 5, which are usually prepared in small quantities, are synthesized with average yields of 80%, using up to 80g of starting material. The mechanism of the chlorination of 4 is investigated computationally for the first time. The results suggest that the chlorination with phosphoryl chloride occurs in an alternating phosphorylation-chlorination manner (pathway 1) which is preferred over a sequence which starts with two phosphorylations. The investigated 4,6-dichloropyrimidines described herein form strong complexes with dichlorophosphoric acid but weak complexes with hydrochloric acid (generated during workup). These latter complexes explain the necessity of using aqueous sodium carbonate during the working up. In order to prevent possible formation of pyrimidinium salts between intermediates or the final dichloropyrimidines and unreacted hydroxypyrimidone, the latter could be deactivated with a strong acid such as dichlorophosphoric acid, thus allowing chlorination but prohibiting salt formation. Because of its general applicability to all nitrogen heterocycle chlorinations with phosphoryl chloride, the proposed route to dichloropyrimidines without solvent or side products, using less toxic reactants, is of general synthetic interest.
- Opitz, Andreas,Sulger, Werner,Daltrozzo, Ewald,Koch, Rainer
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p. 814 - 824
(2015/05/20)
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- Design, synthesis and antifungal activities of novel strobilurin derivatives containing pyrimidine moieties
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Strobilurins are one of the most important classes of agricultural fungicides. To discover new strobilurin derivatives with high activity against resistant pathogens, a series of novel β-methoxyacrylate analogues were designed and synthesized by integrati
- Zhang, Xiang,Gao, Yong-Xin,Liu, Hui-Jun,Guo, Bao-Yuan,Wang, Hui-Li
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p. 2627 - 2634
(2012/10/29)
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- NOVEL IMMUNE SYSTEM MODULATORS
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The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
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Page/Page column 92
(2013/03/14)
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- NOVEL IMMUNE SYSTEM MODULATORS
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The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
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Page/Page column 134
(2013/02/28)
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- N-Substituted Glycine Derivatives: Prolyl Hydroxylase Inhibitors
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The invention described herein relates to certain pyrimidinedione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
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Page/Page column 8
(2008/12/06)
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- NOVEL PYRIMIDINE COMPOUNDS, PROCESS FOR THEIR PREPARATION AND COMPOSITIONS CONTAINING THEM
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The present invention provides new heterocyclic compounds, particularly substituted pyrimidines, methods and compositions for making and using these heterocyclic compounds, and methods for treating a variety of diseases and disease states, including atherosclerosis, arthritis, restenosis, diabetic nephropathy, or dyslipidemia, or disease states mediated by the low expression of Perlecan.
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Page/Page column 249; 292
(2008/06/13)
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- Pyrimidine A2b selective antagonist compounds, their synthesis and use
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The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substitut
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- Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
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This invention is directed to aryl and heterocyclyl substituted pyrimidine derivatives selected from the following formulae: wherein Z1, Z2, R1, R2, R3, R4, R5and R6are defined herein. These compounds are useful as anti-coagulants.
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- 2-aryl-8-oxodihydropurine derivative, process for the producing the same, medicinal compositions containing the same, and intermediates thereof
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2-Aryl-8-oxodihydropurine derivative of the following formula (I): wherein W is H, lower alkyl, halogen, lower alkoxy, amino, mono- or di-lower alkylamino, or substituted or unsubstituted phenyl; X is H, lower alkyl, cycloalkyl-lower alkyl, substituted or unsubstituted phenyl-lower alkyl, lower alkenyl, carbamoyl, di-lower alkylcarbamoyl, or a group of the formula (Q): —CH(R3)CON(R1)(R2); Y is H, lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, lower alkenyl, substituted or unsubstituted phenyl-lower alkyl, or a group of the formula (Q): —CH(R3)CON(R1)(R2); A is substituted or unsubstituted phenyl, or substituted or unsubstituted heteroaryl; provided that when one of X and Y of the above formula (I) is the group of the formula (Q), then the other is the same groups for X or Y as described above except for the group of the formula (Q), or a pharmaceutically acceptable acid addition salt thereof. These compounds are useful for the prophylaxis or treatment of central nervous disorders such as anxiety-related diseases (neurosis, somatoform disorders, anxiety disorders, and others), depression, epilepsy, etc., or circulatory organs disorders such as angina pectoris, hypertension.
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- Gabaa receptor subtypes and methods for screening drug compounds using imidazoquinoxalines and pyrrolopyrimidines to bind to gabaa receptor subtypes
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The present invention provides methods for screening drug compounds utilizing compounds of formulas I and II, where formulas I and II are STR1 and the pharmaceutically acceptable salts thereof where: R 1, R 2, R 3, and R 4 represent hydrogen, halogen, alk
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- Synthesis of 4,6-disubstituted- and 4,5,6-trisubstituted-2-phenyl- pyrimidines and their affinity towards A1 adenosine receptors
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Synthesis and assay of title compounds are reported. The results can support our hypothesis about the possibility that molecules characterized by great flexibility, as the title 2-phenyl-4,5,6-triaminopyrimidines, can better interact with the receptor sites compared with rigid molecules as 2,6,9-trisubstituted 8-azaadenines. Relatively low activity shown by pyrimidine derivatives demonstrated the importance of the bicyclic aromatic system in 8-azaadenines and adenines to give a favourable interaction between a hexogenous molecule and the A1 adenosine receptors.
- Biagi,Giorgi,Livi,Scartoni,Lucacchini
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- CERTAIN ARYL FUSED PYRROLOPYRIMIDINES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS
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The present invention encompasses structures of the formula: STR1 and the pharmaceutically acceptable non-toxic salts thereof wherein: STR2 and X represents hydrogen, halogen, or hydroxy; W represents an aryl group unsubstituted or substituted with
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- CERTAIN CYCLOALKYL AND AZACYCLOALKYL PYRROLOPYRIMIDINES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS
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The invention encompasses a compound of the formula STR1 and the pharmaceutically acceptable non-toxic salts thereof wherein X, W, Y, R, and R2 are variables.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.
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