cas 13036-50-5, 2-CHLORO-4-PHENYLPYRIMIDINE

Articles about 13036-50-5Total 43 be found

Article title
Article abstract
Author
Journal number and time
Download

SPIROPIPERIDINE ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
The present disclosure relates to compounds of formula (I) that are useful as modulators of α7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation.
-
Page/Page column 51-52

(2021/05/15)

Redox deracemization of phosphonate-substituted dihydropyrimidines
An efficient redox deracemization of the phosphonic ester substituted 3,4-dihydropyrimidin-2-one (DHPM) derivatives is described. The one-pot deracemization strategy consisted of the oxidization to destroy the stereocenter center and the following asymmetric transfer hydrogenation to regenerate the chiral carbon center with the vicinal phosphonic ester group, providing a series of optically active phosphonate substituted DHPMs with up to 96% ee.
Feng, Guang-Shou,Guo, Xuan,Meng, Fan-Jie,Shao, Bing-Ru,Shi, Lei,Velopolcek, Maria K.
supporting information
p. 10570 - 10574
(2021/12/27)

P-phenylenediamine LSD1 inhibitor and preparation method thereof
Disclosed are a p-phenylenediamine derivative as represented by general formula I, a pharmaceutically acceptable salt, and a stereoisomer thereof. The p-phenylenediamine derivative as represented by general formula I, the pharmaceutically acceptable salt thereof and the stereoisomer thereof can be used alone or in combination as lysine-specific demethylase-1 (LSD1) inhibitors.
-
Paragraph 0139-0141

(2021/09/08)

Access to Cyanoimines Enabled by Dual Photoredox/Copper-Catalyzed Cyanation of O-Acyl Oximes
An efficient strategy for the synthesis of pharmaceutically important and synthetically useful cyanoimines, as well as cyanamides, has been described. This strategy is enabled by dual photoredox/copper-catalyzed cyanation of O-acyl oximes or O-acyl hydroxamides. This state of the art protocol for cyanoimines and cyanamides features readily available starting materials, mild reaction conditions, good functional group tolerance, and operational simplicity. The resultant cyanoimines can be transformed into structurally diverse and functionally important N-containing heterocycles.
Wei, Ziyan,Yu, Shouyun,Zhang, Ai Hua,Zhang, Hao
p. 7315 - 7320
(2020/10/02)

A sustainable heterogenized palladium catalyst for Suzuki-Miyaura cross coupling reaction of azaheteroaryl halides in aqueous media
A unique recyclable Pd catalyst (‘SiO2’-NH2-Pd) for Suzuki-Miyaura coupling reaction of azaheteroaryl halides is developed. The catalytic system is working under mild aqueous condition with low Pd loading and without the use of phosphine ligand. The plausible mechanism is proposed based on the formation of undesired symmetrical biaryl from the coupling reaction of azaheteroaryl chlorides due to the oxidative homocoupling of nucleophilic arylboronic acid. This catalytic system represents an attractive and promising approach for the synthesis of azaheterobiaryls with high product yields. The catalyst has demonstrated an excellent recyclability.
Ganesamoorthy,Muthu Tamizh,Shanmugasundaram,Karvembu
p. 76 - 85
(2018/03/23)

Design, synthesis and biological evaluation of pyrimidine-based derivatives as VEGFR-2 tyrosine kinase inhibitors
Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a crucial role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has already become an attractive approach for cancer therapy. In this study, a novel pyrimidine-based derivative 7j was designed as lead compound, and three series of potent VEGFR-2 inhibitors were synthesized and biologically evaluated against A549 and HepG2 cell lines. Compounds 7d, 9s and 13n exhibited superior inhibitory activities against A549 cell with IC50 ranged from 9.19 to 13.17 μM and HepG2 cell with IC50 ranged from 11.94 to 18.21 μM compared to those of Pazopanib (IC50 = 21.18 and 36.66 μM). In addition, molecular docking study was performed to investigate the binding capacity and binding mode between target compounds and VEGFR-2.
Sun, Wuji,Hu, Shengquan,Fang, Shubiao,Yan, Hong
p. 393 - 405
(2018/04/23)

Identification of N-arylsulfonylpyrimidones as anticancer agents
For confirming the role of five membered ring of imidazolidinone moiety of N-arylsulfonylimidazolidinones (7) previously reported with highly potent anticancer agent, a series of N-arylsulfonylpyrimidones (10a–g) and N-arylsulfonyltetrahydropyrimidones (11a–e) were prepared and their anti-proliferating activity was measured against human cancer cell lines (renal ACHN, colon HCT-15, breast MDA-MB-231, lung NCI-H23, stomach NUGC-3, and prostate PC-3) using XTT assay. Among them, 1-(1-acetylindolin-5-ylsulfonyl)-4-phenyltetrahydropyrimidin-2(1H)-one (11d, mean GI50?=?3.50?μM) and ethyl 5-(2-oxo-4-phenyltetrahydropyrimidin-1(2H)-ylsulfonyl)-indoline-1-carboxylate (11e, mean GI50?=?0.26?μM) showed best growth inhibitory activity against human cancer cell lines. Considering the activity results, N-arylsulfonyltetrahydropyrimidones (11) exhibited more potent activity compared to N-arylsulfonylpyrimidones (10) and comparable activity to N-arylsulfonylimidazolidinones (7). Especially, tetrahydropyrimidin-2(1H)-one analogs containing acylindolin-5-ylsulfonyl moiety at position 1 demonstrated their strong growth inhibitory activity against human cancer cell lines.
Subramanian, Santhosh,Boggu, Pulla Reddy,Yun, Jieun,Jung, Sang-Hun
p. 251 - 258
(2018/03/09)

METHODS AND COMPOSITIONS OF INHIBITING DCN1-UBC12 INTERACTION
In one aspect, the invention relates to substituted l-phenyl-3-(piperidin-4-yl)urea analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the DCN1-UBC12 interaction inhibitors of DCN1 -mediated cullin-RING ligase activity, methods of making same, pharmaceutical compositions comprising same, methods of treating disorders using the disclosed compounds and compositions, methods of treating disorders associated with a DCN1-UBC12 interaction dysfunction, methods of treating disorders associated with a DCN1-mediated cullin-RING ligase activity dysfunction, methods of male contraception comprising the disclosed compounds and compositions, and kits comprising the disclosed compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
-
Paragraph 00469

(2017/04/11)

Synthesis and evaluation of the NSCLC anti-cancer activity and physical properties of 4-aryl-N-phenylpyrimidin-2-amines
Reported herein are efforts to profile 4-aryl-N-phenylpyrimidin-2-amines in terms of their anti-cancer activity towards non small-cell lung carcinoma (NSCLC) cells. We have synthesized new 4-aryl-N-phenylpyrimidin-2-amines and assessed them in terms of their cytotoxicity (A549, NCI-H187, MCF7, Vero & KB) and physicochemical properties (logD7.4 and solubility). 13f and 13c demonstrated potent anti-cancer activity in A549 cells (0.2 μM), compared to 0.4 μM for the NSCLC drug Doxorubicin. 13f also displayed low experimental logD7.4 (2.9) and the best solubility (～40 μM). Compounds 13b and 13d showed the best balance of A549 anti-cancer activity and selectivity. 13g showed good activity and selectivity comparable with the anti-cancer drug Doxorubicin.
Toviwek, Borvornwat,Suphakun, Praphasri,Choowongkomon, Kiattawee,Hannongbua, Supa,Gleeson, M. Paul
supporting information
p. 4749 - 4754
(2017/09/29)

Novel Compounds
The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C- terminal hydrolase 30 or Ubiquitin Specific Peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (I): (I) or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c, R1d, R1e, R1f, R1g, R2, X, L and A are as defined herein.
-
Page/Page column 54

(2017/07/06)

Catalyst Selection Facilitates the Use of Heterocyclic Sulfinates as General Nucleophilic Coupling Partners in Palladium-Catalyzed Coupling Reactions
A range of 5- and 6-membered heterocycle-derived sulfinates are shown to be effective nucleophilic coupling partners with aryl chlorides and bromides using Pd(0) catalysis. The use of optimal reaction conditions, specifically incorporating a P(t-Bu)2Me-derived Pd catalyst, allowed reactions to be performed at moderate temperatures and enabled the inclusion of a variety of sensitive functional groups. Challenging heterocyclic sulfinates, including pyrazine, pyridazine, pyrimidine, pyrazole, and imidazole, were all shown to perform well.
Markovic, Tim,Rocke, Benjamin N.,Blakemore, David C.,Mascitti, Vincent,Willis, Michael C.
supporting information
p. 6033 - 6035
(2017/11/27)

New organic electroluminescent compounds and the use of the compound of the organic electroluminescent device
Provided are a novel organic electroluminescent compound and an organic electroluminescent device using the same. When used as a host material of an organic electroluminescent material of an OLED device, the organic electroluminescent compound disclosed herein exhibits good luminous efficiency and excellent life property as compared to the existing host material. Therefore, it may be used to manufacture OLEDs having very superior operation life.
-
Paragraph 0067; 0084; 0085

(2016/10/07)

Compounds with cardiac myosin activating function and pharmaceutical composition containing the same for treating or preventing heart failure
The present invention relates to a compound having a cardiotonic activating function and a pharmaceutical composition containing the same. The composition comprising the compound according to the present invention is effective in preventing or treating heart failure. In addition, the compound is represented by chemical formula 2 or is pharmaceutically acceptable salt thereof.COPYRIGHT KIPO 2016
-
Paragraph 0700-0702

(2017/02/02)

Novel organic electroluminescent compounds and organic electroluminescent device using the same
The present invention relates to a novel organic light-emitting compound and an organic electroluminescent device containing the same. More specifically, the organic light-emitting compound according to the present invention is selected from the following chemical formula 1 to 6. andlt;Img id = andPrime;i0030andPrime; he = andPrime;86andPrime; wi = andPrime;125andPrime; file = andPrime;pat00030.jpgandPrime; img-format = andPrime;jpgandPrime; /andgt; [In formula 1 to 6, X and Y are each independently selected from N (R_1), C (R_2) (R_3) and Si (R_4) (R_5), wherein one of either X or Y must be N (R_1); the other is C (R_2) (R_3) or Si (R_4) (R_5); and Z_1 to Z_8 are each independently selected from C (R_6) and N, wherein R_6 can be different from each other and adjacent R_6 may be bonded to each other to form a ring.] The organic light-emitting compound according to the present invention is used as a host material of the organic light-emitting material in OLED devices and shows good luminous efficiency and excellent life properties of material, compared with conventional host materials, thereby being advantageous in producing an OLED having a very good operating life.COPYRIGHT KIPO 2015
-
Paragraph 0059; 0076; 0077

(2017/04/14)

HETEROCYCLIC COMPOUNDS AND USE OF SAME
Novel heterocyclic compounds are provided which display useful efficacy in the treatment of diseases caused by trypanosomatids. Particularly, the compounds of the invention are useful in the treatment of HAT and/or Chagas disease and/or Animal African trypanosomiasis (AAT).
-
Paragraph 00186

(2016/01/08)

Compounds with cardiac myosin activating function and pharmaceutical composition containing the same for treating or preventing heart failure
Disclosed are a compound having cardiotonic activity and a pharmaceutical composition containing the same, and the composition containing the compound, according to the present invention, is useful for preventing and treating heart failure.COPYRIGHT KIPO 2016
-
Paragraph 0700-0702

(2016/10/07)

Heat shock protein 70 inhibitors. 2. 2,5′-thiodipyrimidines, 5-(phenylthio)pyrimidines, 2-(pyridin-3-ylthio)pyrimidines, and 3-(phenylthio)pyridines as reversible binders to an allosteric site on heat shock protein 70
The discovery and development of heat shock protein 70 (Hsp70) inhibitors is currently a hot topic in cancer. In the preceding paper in this issue (10.1021/jm401551n), we have described structure-activity relationship studies in the first Hsp70 inhibitor class rationally designed to bind to a novel allosteric pocket located in the N-terminal domain of the protein. These ligands contained an acrylamide to take advantage of an active cysteine embedded in the allosteric pocket and acted as covalent protein modifiers upon binding. Here, we perform chemical modifications around the irreversible inhibitor scaffold to demonstrate that covalent modification is not a requirement for activity within this class of compounds. The study identifies derivative 27c, which mimics the biological effects of the irreversible inhibitors at comparable concentrations. Collectively, the back-to-back manuscripts describe the first pharmacophores that favorably and selectively interact with a never explored pocket in Hsp70 and provide a novel blueprint for a cancer-oriented development of Hsp70-directed ligands.
Taldone, Tony,Kang, Yanlong,Patel, Hardik J.,Patel, Maulik R.,Patel, Pallav D.,Rodina, Anna,Patel, Yogita,Gozman, Alexander,Maharaj, Ronnie,Clement, Cristina C.,Lu, Alvin,Young, Jason C.,Chiosis, Gabriela
p. 1208 - 1224
(2014/03/21)

Discovery of 2-(cyclohexylmethylamino)pyrimidines as a new class of reversible valosine containing protein inhibitors
Valosine-containing protein (VCP), also known as p97 or cdc48 in yeast, is a highly abundant protein belonging to the AAA ATPase family involved in a number of essential cellular functions, including ubiquitin-proteasome mediated protein degradation, Golgi reassembly, transcription activation, and cell cycle control. Altered expression of VCP has been detected in many cancer types sometimes associated with poor prognosis. Furthermore, VCP mutations are causative of some neurodegenerative disorders. In this paper we report the discovery, synthesis, and structure-activity relationships of substituted 2-aminopyrimidines, representing a new class of reversible VCP inhibitors. This class of compounds, identified in a HTS campaign against recombinant VCP, has been progressively expanded and manipulated to increase biochemical potency and gain cellular activity.
Cervi, Giovanni,Magnaghi, Paola,Asa, Daniela,Avanzi, Nilla,Badari, Alessandra,Borghi, Daniela,Caruso, Michele,Cirla, Alessandra,Cozzi, Liviana,Felder, Eduard,Galvani, Arturo,Gasparri, Fabio,Lomolino, Antonio,Magnuson, Steven,Malgesini, Beatrice,Motto, Ilaria,Pasi, Maurizio,Rizzi, Simona,Salom, Barbara,Sorrentino, Graziella,Troiani, Sonia,Valsasina, Barbara,O'Brien, Thomas,Isacchi, Antonella,Donati, Daniele,D'Alessio, Roberto
p. 10443 - 10454
(2015/02/19)

NOVEL ORGANIC ELECTROLUMINESCENT COMPOUNDS AND ORGANIC ELECTROLUMINESCENT DEVICE USING THE SAME
Provided are organic electroluminescent compounds of a fused pentacyclic structure of general formula I, and an organic electroluminescent device using said compounds. Since the organic electroluminescent compounds exhibit good luminous efficiency and lifespan, they may be used to manufacture OLED devices which have a superior operational lifetime and also have low power consumption due to the improved power efficiency of the compounds.
-
Page/Page column 19

(2011/08/21)

HEAT SHOCK PROTEIN BINDING COMPOUNDS, COMPOSITIONS, AND METHODS FOR MAKING AND USING SAME
The present subject matter relates to a compound represented by the general formula (I) or (I') or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70).
-
Page/Page column 167

(2011/04/13)

NOVEL PYRROLIDINE DERIVED BETA 3 ADRENERGIC RECEPTOR AGONISTS
The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.
-
Page/Page column 46-47

(2011/04/14)

Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit
A bis-amide antagonist of Smoothened, a seven-transmembrane receptor in the Hedgehog signaling pathway, was discovered via high throughput screening. In vitro and in vivo experiments demonstrated that the bis-amide was susceptible to N-acyl transferase mediated amide scission. Several bioisosteric replacements of the labile amide that maintained in vitro potency were identified and shown to be metabolically stable in vitro and in vivo.
Brown, Matthew L.,Aaron, Wade,Austin, Richard J.,Chong, Angela,Huang, Tom,Jiang, Ben,Kaizerman, Jacob A.,Lee, Gary,Lucas, Brian S.,McMinn, Dustin L.,Orf, Jessica,Rong, Minqing,Toteva, Maria M.,Xu, Guifen,Ye, Qiuping,Zhong, Wendy,Degraffenreid, Michael R.,Wickramasinghe, Dineli,Powers, Jay P.,Hungate, Randall,Johnson, Michael G.
scheme or table
p. 5206 - 5209
(2011/10/09)

Convenient preparation of 4-aryl-2-(heteroarylamino)pyrimidines and 4-anilino-2-(heteroarylamino)pyrimidines
4-Aryl-2-anilinopyrimidines and 2,4-dianilinopyrimidines are privileged structures found in many drug-like molecules and biologically active compounds. A method for the quick assembly of novel 4-aryl- and 4-anilino-2-(heteroarylamino)pyrimidines via Buchwald-Hartwig N-arylations at elevated temperatures under sealed tube conditions is reported. This method's convenience and practicality is demonstrated through the preparation of several novel non-nucleoside reverse transcriptase inhibitor (NNRTI) analogues.
Bliss, Brian I.,Ahmed, Feryan,Iyer, Subashree,Lin, Weimin,Walker, Joel,Zhao, He
supporting information; experimental part
p. 3259 - 3262
(2010/07/10)

One-pot double Suzuki couplings of dichloropyrimidines
An effective one-pot, regioselective double Suzuki coupling of 2,4-dichloropyrimidine has been developed, which enables the quick and efficient synthesis of diarylated pyrimidines. The choice of solvent proved critical to the success of this reaction sequence, with alcoholic solvent mixtures affording much greater reactivity and requiring correspondingly lower temperatures than the use of polar aprotic solvents. Georg Thieme Verlag Stuttgart.
Anderson, Samantha C.,Handy, Scott T.
experimental part
p. 2721 - 2724
(2010/10/19)

Direct C-H bond arylation of (Hetero)arenes with Aryl and heteroarylboronic acids
A novel microwave-promoted protocol mediated by Mn(OAc)3 was developed for the single-electron-transfer oxidative direct C-H bond arylation of (hetero)arenes with aryl and hetero-arylboronic acids. Various electron-deactivated and electron-rich heteroarenes and benzene underwent successfully the direct arylation in this general process. The use of slight excess of heteroarene or benzene in this method was found to be sufficient. Georg Thieme Verlag Stuttgart New York.
Guchhait, Sankar K.,Kashyap, Maneesh,Saraf, Shuddham
experimental part
p. 1166 - 1170
(2010/06/11)

SUBSTITUTED PYRIMIDINYL-AMINES AS PROTEIN KINASE INHIBITORS
The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.
-
Page/Page column 48; 49

(2009/04/25)

Simple microwave-assisted ligand-free Suzuki cross-coupling: Functionalization of halo-pyrimidine moieties
(Chemical Equation Presented) An advantageous ligand-free protocol for Suzuki couplings is described. The synthetic procedure entails microwave irradiation for the reduction of the reaction times and the use of silica cartridges for the purification. Dihalo-pyrimidine structures, interesting scaffolds in medicinal chemistry, were chosen as test compounds.
Colombo, Matteo,Giglio, Marco,Peretto, Ilaria
p. 1077 - 1081
(2008/12/20)

Inhibitors of Hepatitis C Virus
Macrocyclic peptides are disclosed having the general formula: wherein R3, R3′, R4, R6, R′, X, Q and W are described. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
-
Page/Page column 64

(2008/12/04)

Inhibitors of Hepatitis C Virus
Macrocyclic peptides are disclosed having the general formula: wherein R3, R3′, R4, R6, R′, X, Q and W are described. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
-
Page/Page column 60

(2008/12/04)

Inhibitors of Hepatitis C Virus
Macrocyclic peptides are disclosed having the general formula: wherein R3, R′3, R4, R6, R′, X, Q and W are described. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
-
Page/Page column 63

(2008/12/04)

Hepatitis C virus inhibitors
Macrocyclic peptides are disclosed having the general formula: wherein R′, R3, R3′, R4, R6, X, Q, and W are described. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
-
Page/Page column 65

(2010/11/26)

SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE
The present invention relates to pyridines, pyrimidines and derivatives thereof, and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic beta cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.
-
Page/Page column 69

(2010/10/20)

Microwave-assisted, efficient and regioselective Pd-catalyzed C-phenylation of halopyrimidines
We herein report that flash heating microwave irradiation is a helpful tool in the formation of arylpyrimidines from the corresponding halopyrimidines. The palladium-catalyzed cross-coupling reactions of 2,4-di- and 2,4,5-trihalopyrimidines with phenylboronic acid under the above conditions are described. By use of the appropriate catalyst and the adequate halopyrimidine, good regioselectivity can be achieved in the 2-, 4-, or 5-positions of the heterocycle. In addition, we show that this methodology is ameneable for the stepwise preparation of mono-, di-, and triphenylpyrimidines.
Ceide, Susana Conde,Montalban, Antonio Garrido
p. 4415 - 4418
(2007/10/03)

Synthesis and SAR of highly potent and selective dopamine D 3-receptor antagonists: 1H-Pyrimidin-2-one derivatives
The synthesis and SAR of novel highly potent and selective dopamine D 3-receptor antagonists based on a 1H-pyrimidin-2-one scaffold are described. A-690344 antagonized PD 128907-induced huddling deficits in rat (ED50 6.1 mg/kg po), a social interaction paradigm.
Geneste, Herve,Backfisch, Gisela,Braje, Wilfried,Delzer, Juergen,Haupt, Andreas,Hutchins, Charles W.,King, Linda L.,Kling, Andreas,Teschendorf, Hans-Juergen,Unger, Liliane,Wernet, Wolfgang
p. 490 - 494
(2007/10/03)

SUBSTITUTED N-HETEROCYCLIC COMPOUNDS AND THEIR USE AS DOPAMINE D3 RECEPTOR LIGANDS
The invention relates to the substituted N-heterocyclic compounds of general formula (I), wherein Ar, A1, X, Y, A2 and Q are defined as in claim 1, and to the tautomers of the compounds (I), the physiologically acceptable salts of compounds (I) and the physiologically acceptable salts of the tautomers of compound (I). The invention also relates to the use of these compounds and their pharmacologically acceptable salts in the production of a pharmaceutical agent for treating diseases that respond to the influence exerted by dopamine D3 receptor ligands, especially for treating diseases of the central nervous system, especially schizophrenia and/or depression.
-
Page/Page column 74-75

(2008/06/13)

Hepatitis C virus inhibitors
The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which inhibit the function of the NS3 protease (also referred to herein as “serine protease”) encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS3 protease.
-
Page/Page column 76

(2008/06/13)

PYRIMIDIN-2-ONE COMPOUNDS AND THEIR USE AS DOPAMINE D3 RECEPTOR LIGANDS
The invention relates to pyrimidin-2-one compounds of general formula (I), in addition to the derivatives and tautomers of (I) and the physiologically acceptable salts of said compounds. In said formula: A represents linear or branched C3-C6 alkene, which can have a double bond or triple bond and/or a group Z, which is not adjacent to the nitrogen atom of the pyrimidinone ring and is selected from O, S, C(O), NR3, C(O)NR3, NR3C(O), OC(O) and C(O)O; B represents a group of formula (II), in which X stands for CH2 or N and Y stands for CH2 or CH2CH2, or X-Y can also jointly represent C=CH, C=CH-CH2 or CH-CH=CH; R1 and R 2 are defined as cited in the description and the claims; and Ar represents an optionally substituted aromatic group. The invention also relates to a pharmaceutical agent, containing at least one compound (I) and the tautomers, derivatives and/or acid addition salts of said compound, optionally together with physiologically acceptable carriers and/or auxiliary agents. The invention also relates to the use of compounds of formula (I), and their tautomers, derivatives and pharmacologically acceptable acid addition salts for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor ligands.
-
Page 64; 65

(2010/02/08)

HEPATITIS C VIRUS INHIBITORS
Hepatitis C virus inhibitors are disclosed having the general formula:(I) wherein R1, R2, R3, R', B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds toinhibit HCV are also disclosed.
-
Page 442

(2008/06/13)

Syntheses of substituted pyridines, quinolines and diazines via palladium-catalyzed cross-coupling of aryl Grignard reagents
The palladium-catalyzed cross-coupling reactions between arylmagnesium halides (phenylmagnesium chloride, mesitylmagnesium bromide, 4-(methoxycarbonyl)phenylmagnesium chloride and 4-cyanophenylmagnesium chloride) and halopyridines allowed the synthesis of substituted pyridines. Owing to the remarkably mild conditions used (often below 0°C), the reaction could be extended to the use of functionalized halopyridines, haloquinolines and halodiazines.
Bonnet, Véronique,Mongin, Florence,Trécourt, Fran?ois,Quéguiner, Guy,Knochel, Paul
p. 4429 - 4438
(2007/10/03)

Synthesis of indolylpyrimidines via cross-coupling of indolylboronic acid with chloropyrimidines facile synthesis of meridianin D
Palladium catalyzed cross-coupling reaction of 3-indolylboronic acid with 2,4-dichloropyrimidines proceeded regioselectively to yield indolyl-or bis(indolyl)pyrimidines in high yield, depending on the projection of 3indolylboronic acid. The marine indole alkaloid meridianin D and an analogue were synthesised via the palladium catalyzed cross-coupling reaction as a key step.
Jiang, Biao,Yang, Cai-Guang
p. 1489 - 1498
(2007/10/03)

Regiochemistry in Pd-Catalysed Organotin Reactions with Halopyrimidines
Chlorines in activated pyrimidine position is replaced by carbon substituents in Pd-catalysed reactions with organotin compounds.The 4(6)-position is more reactive than the 2-position allowing for regioselective coupling in 2,4(6)-dihalopyrimidines.A bromine substituent is required for coupling in the benzenoid 5-position.In 5-bromo-2,4-dichloropyrimidine the 4-chlorine is replaced before the 5-bromine and the latter before the 2-chloro substituent, all in a regioselective manner.The methodology can be used to introduce functionalized carbon substituents into any pyrimidine position.
Solberg, Jan,Undheim, Kjell
p. 62 - 68
(2007/10/02)

Addition and Substitution Reactions of Chloropyrimidines with Lithium Reagents
-
Harden, Donald B.,Mokrosz, Maria J.,Strekowski, Lucjan
p. 4137 - 4140
(2007/10/02)

Transformations of 2-Aminopyrimidines and Their N-Oxides under Diazotation Conditions
The diazotation of 2-aminopyrimidines and their N-oxides in solutions with various acidities was studied.It is shown that the amino group in pyrimidine N-oxides is not diazotized in strongly acidic media and that bromination in the 5 position of the pyrimidine ring is observed in concentrated hydrobromic acid.When the reaction was carried out in moderately acidic media, it was possible to synthesize the difficult-to-obtain 2-halopyrimidine N-oxides.
Sedova, V. F.,Mustafina, T. Yu.,Krivopalov, V. P.,Mamaev, V. P.
p. 91 - 94
(2007/10/02)