13051-89-3Relevant academic research and scientific papers
Synthesis and reactivity of a 1,4-dihydropyrazine derivative
Rodrigues, Anabela,Ferreira, Paula M.T.,Monteiro, Luís S.
, p. 8489 - 8496 (2004)
N,N-Bis-(tert-butoxycarbonyl)-2,5-bis-methoxycarbonyl-1,4-dihydropyrazine can be obtained in high yield by treatment of the methyl ester of N-(4-toluenesulfonyl)-N-(tert-butoxycarbonyl)-α,β-didehydroalanine with dimethylaminopyridine and potassium carbona
TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS HAVING A PYRIDINE OR PYRAZINE MOIETY, CONJUGATES THEREOF, AND METHODS AND USES THEREFOR
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Paragraph 0137, (2019/02/28)
Compounds having a structure according to formula (I) where R1 and Ar are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
Self-Assembly of Cyclohelicate [M3L3] Triangles Over [M4L4] Squares, Despite Near-Linear Bis-terdentate L and Octahedral M
Hogue, Ross W.,Dhers, Sébastien,Hellyer, Ryan M.,Luo, Jingwei,Hanan, Garry S.,Larsen, David S.,Garden, Anna L.,Brooker, Sally
supporting information, p. 14193 - 14199 (2017/10/07)
Self-assembly of 1:1:2 MII(BF4)2 (M=Zn or Fe), pyrazine-2,5-dicarbaldehyde (1) and 2-(2-aminoethyl)pyridine gave trimetallic triangle architectures rather than the anticipated tetrametallic [2×2] squares. Options for the n
DOPAMINE D3 RECEPTOR ANTAGONISTS COMPOUNDS
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Page/Page column 126, (2016/05/19)
The disclosure is directed to novel dopamine D3 receptor antagonists, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, including treating drug dependency and psychosis.
Quaternary Stereogenic Centers through Enantioselective Heck Arylation of Acyclic Olefins with Aryldiazonium Salts: Application in a Concise Synthesis of (R)-Verapamil
Oliveira, Caio C.,Pfaltz, Andreas,Correia, Carlos Roque Duarte
supporting information, p. 14036 - 14039 (2016/01/25)
We describe herein a highly regio- and enantioselective Pd-catalyzed Heck arylation of unactivated trisubstituted acyclic olefins to provide all-carbon quaternary stereogenic centers. Chiral N,N ligands of the pyrimidine- and pyrazino-oxazoline class were developed for that purpose, providing the desired products in good to high yields with enantiomeric ratios up to >99:1. Both linear and branched substituents on the olefins were well-tolerated. The potential of this new method is demonstrated by the straightforward synthesis of several O-methyl lactols and lactones containing quaternary stereocenters, together with a concise enantioselective total synthesis of the calcium channel blocker verapamil.
Design, synthesis, and biological evaluation of bone-targeted proteasome inhibitors for multiple myeloma
Agyin, Joseph K.,Santhamma, Bindu,Roy, Sudipa S.
supporting information, p. 6455 - 6458 (2013/11/19)
Multiple myeloma (MM) is an incurable neoplasm characterized by devastating and progressive bone destruction. Standard chemotherapeutic agents have not been effective at significantly prolonging the survival of MM patients and these agents are typically a
Dinuclear copper(II) complexes of two homologous pyrazine-based bis(terdentate) diamide ligands
Klingele, Julia,Moubaraki, Boujemaa,Murray, Keith S.,Boas, John F.,Brooker, Sally
, p. 1530 - 1541 (2007/10/03)
The 1:1 reactions of the new bis(terdentate) diamide ligand N, N′-bis(2-pyridylmethyl)pyrazine-2,5-dicarboxamide (H2L 1) and its higher homologue N,N′-bis[2-(2-pyridyl)ethyl] pyrazine-2,5-dicarboxamide (H2L2) with Cu(BF 4)2·4H2O in the absence of added base have consistently afforded dicopper(II) complexes of the doubly deprotonated ligands (L1)2- and (L2)2-. The complex [CuII2(L2)(H2O) 2(MeCN)2](BF4)2 (2a) has been structurally characterised. Subsequently, reactions employing a correct stoichiometric 2:1 metal-to-ligand ratio in MeCN have afforded bulk samples of the dinuclear complexes. The compounds [CuII2(L 1)(MeCN)2(H2O)2)(BF 4)2·H2O (1a·H2O) and [CuII2(L2)(H2O)4(BF 4)2]-2H2O (2b-2H2O) have been structurally characterised. While complex 1a-H2O of the lower ligand homologue exhibits very weak antiferromagnetic spin coupling (J = -0.24 cm -1), complex 2b of the higher ligand homologue exhibits very weak ferromagnetic spin coupling (J = +0.67 cm-1). EPR studies have been carried out on polycrystalline powders and frozen DMF solutions of 1a-H 2O and 2b·2H2O. The EPR spectra of the polycrystalline powders indicate the presence of dipolar broadening and weak intermolecular exchange, while those of the frozen DMF solutions are characteristic of dipolar-coupled CuII pairs within the dinuclear molecules, with no evidence of intraor intermolecular exchange. The spectral simulations confirm that the binuclear structure and the Cu...Cu distances are retained in frozen solution. Dinuclear SiF22- containing compounds, [CuII2(L1)(H2O) 4](SiF6) (1b) and [[CuII2(L 1)(H2O)2(μSiF6))·4H 2O]∞ (1c-4H2O). were obtained serendipitously, in nearly quantitative yield, by the 2:1 reaction of Cu(BF 4)2· 4H2O with H2L 1 in H2O. The unexpected SiF62- anions were generated in the course of the reaction by partial hydrolysis of the BF4- anions employed, thus forming traces of HF which reacted with the glassware.
Stereoisomeric tricyclic bis(dioxopiperazines) and pharmaceutical compositions
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, (2008/06/13)
Stereoisomeric tricyclic bis(dioxopiperazines) of the formula STR1 wherein R is H or STR2 and the processes for the synthesis thereof are provided. The compounds are effective as antitumor or antimetastatic drugs.
