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Iron-Mediated Electrophilic Amination of Organozinc Halides using Organic Azides

A wide range of alkyl-, aryl- and heteroarylzinc halides were aminated with highly functionalized alkyl, aryl, and heterocyclic azides. The reaction proceeds smoothly at 50 C within 1 h in the presence of FeCl3 (0.5 equiv) to furnish the corresponding secondary amines in good yields. This method was extended to peptidic azides and provided the arylated substrates with full retention of configuration. To demonstrate the utility of this reaction, we prepared two amine derivatives of pharmaceutical relevance using this iron-mediated electrophilic amination as the key step.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1712 – PubChem

 

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141-30-0, Name is 3,6-Dichloropyridazine, belongs to pyridazine compound, is a common compound. SDS of cas: 141-30-0In an article, once mentioned the new application about 141-30-0.

3-[(6-Arylamino)pyridazinylamino]benzoic acids: Design, synthesis and in vitro evaluation of anticancer activity

A series of novel substituted 3,6-disubstituted pyridazines based on the structure of vatalanib (PTK787) were designed and synthesized. The cytotoxicity of the final compounds was tested in vitro on HT-29 colon cancer cell line. Compounds 2a and 2b with 4-chlorophenylamino moiety, exerted the highest cytotoxic activity with IC50 values equal to 15.3 and 3.9 muM respectively. The most promising compound, 2b, was found to be about fivefold more active than vatalanib against HT-29 colon cancer cell line.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1585 – PubChem

 

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NEW COMPOUNDS

The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, geometrical isomers, racemates, tautomers, optical isomers and N-oxides thereof. The invention also relates to pharmaceutical compositions comprising these compounds, and to the use of these compounds for the prophylaxis and treatment of medical conditions relating to disorders of the G-protein-coupled receptor GPR119, such as diabetes and obesity.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1480 – PubChem

 

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Related Products of 141-30-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.141-30-0, Name is 3,6-Dichloropyridazine, molecular formula is C4H2Cl2N2. In a Patent,once mentioned of 141-30-0

2,5,-diazabicyclo[2.2.1]heptane derivatives, their preparation and therapeutic uses

The invention relates to 2,5-diazabicyclo[2.2.1]heptane derivatives, to pharmaceutical compositions containing them, and to methods for the treatment or prevention of disorders associated with a dysfunction of the nicotinic receptors utilizing them.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1439 – PubChem

 

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Related Products of 141-30-0, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.141-30-0, Name is 3,6-Dichloropyridazine, molecular formula is C4H2Cl2N2. In a article,once mentioned of 141-30-0

Pyridazinone compound, preparation method thereof, pharmaceutical composition and its use (by machine translation)

The invention belongs to the field of pharmaceutical chemistry. Specifically, the invention relates to a kind of the following formula I indicated by the pyridazinone compound or its isomer or its pharmaceutically acceptable salt, ester, prodrug or solvate thereof, its preparation method, pharmaceutical composition and its tyrosine kinase inhibitors, in particular inhibitors of c – Met in use. The compound or its pharmaceutical composition as tyrosine kinase inhibitors, in particular as c – Met inhibitors can be used for preventing and/or treating abnormal c – Met related tumor diseases. (by machine translation)

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1353 – PubChem

 

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Original 2-(3-Alkoxy-1 H -pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH)

Following our discovery of human dihydroorotate dehydrogenase (DHODH) inhibition by 2-(3-alkoxy-1H-pyrazol-1-yl)pyrimidine derivatives as well as 2-(4-benzyl-3-ethoxy-5-methyl-1H-pyrazol-1-yl)-5-methylpyridine, we describe here the syntheses and evaluation of an array of azine-bearing analogues. As in our previous report, the structure-activity study of this series of human DHODH inhibitors was based on a phenotypic assay measuring measles virus replication. Among other inhibitors, this round of syntheses and biological evaluation iteration led to the highly active 5-cyclopropyl-2-(4-(2,6-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-3-fluoropyridine. Inhibition of DHODH by this compound was confirmed in an array of in vitro assays, including enzymatic tests and cell-based assays for viral replication and cellular growth. This molecule was found to be more active than the known inhibitors of DHODH, brequinar and teriflunomide, thus opening perspectives for its use as a tool or for the design of an original series of immunosuppressive agent. Moreover, because other series of inhibitors of human DHODH have been found to also affect Plasmodium falciparum DHODH, all the compounds were assayed for their effect on P. falciparum growth. However, the modest in vitro inhibition solely observed for two compounds did not correlate with their inhibition of P. falciparum DHODH.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1803 – PubChem

 

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Antihypertensives. N-1H-pyrrol-1-yl-3-pyridazinamines

The hypothesis that the side effects of hydralazine, such as mutagenicity and lupus erythematosus like syndrome, might be due to the NHNH2 group prompted us to incorporate part of this moiety into pyrrole ring. Therefore, we prepared a series of N-1H-pyrrol-1-yl-3-pyridazinamines and a limited number of N-1H-pyrrol-1-yl-1-phthalazinamines by reaction of 3-hydrazinopyridazines and 1-hydrazinophthalazines with gamma-diketones. Most of these compounds, especially in the pyridazine series, showed moderate to strong antihypertensive activity in spontaneously hypertensive rats. The decrease in blood pressure generally had a slow onset after either oral or intravenous administration. N-(2,5-Dimethyl-1H-pyrrol-1-yl)-6-(4-morpholinyl)-3-pyridazinamine hydrochloride (MDL 899) showed no mutagenic activity in several tests and is now in clinical trials in patients.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1614 – PubChem

 

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Rapid analogue synthesis of trisubstituted triazolo[4,3-b]pyridazines

A rapid analogue synthesis of biologically active 3,6,7-trisubstituted 1,2,4-triazolo[4,3-b]pyridazines was devised to give easy and selective variation of the three substituents through combinations of silicon-directed anion formation, palladium-catalysed couplings and S(N)Ar displacements. (C) 2000 Elsevier Science Ltd.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1654 – PubChem

 

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Application of 141-30-0, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 141-30-0, molcular formula is C4H2Cl2N2, introducing its new discovery.

VASOCONSTRICTIVE DIHYDROBENZOPYRAN DERIVATIVES

The present invention is concerned with compounds of formula STR1 the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R 1 is hydrogen or C. sub.1-6 alkyl; R 2 is hydrogen or C 1-6 alkyl; R. sup.3 is hydrogen or C 1-6 alkyl; R 4 is hydrogen, halo, C 1-6 alkyl, hydroxy, C 1-6 alkyloxy, aryloxy or arylmethoxy; R 5 and R 6 designate R 5a and R 6a wherein R 5a and R 6a taken together form a bivalent radical; or R 5 and R 6 can designate R. sup.5b and R. sup.6b wherein R 5b is hydrogen and R 6b is a heterocycle or an optionally substituted alkenyl or alkynyl group; or R. sup.5 and R 6 designate R 5c and R 6c, wherein R. sup.5c and R 6c are hydrogen, halo, C 1-6 alkyl, C 3-6 alkenyl, C 3-6 alkynyl, hydroxy, C 1-6 alkyloxy, cyano, aminoC. sub.1-6 alkyl, carboxyl, C 1-6 alkyloxycarbonyl, nitro, amino, aminocarbonyl, C 1-6 alkylcarbonylamino, or mono-di(C 1-6 alkyl)amino; Q is a heterocyclic ring containing at least one nitrogen atom or a radical of formula STR2 pharmaceutical compositions, preparations and use as a medicine are also described.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1549 – PubChem

 

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Alkoxyalkylidenhydrazinopridazines and process for their preparation

There are described new alkoxyalkylidenhydrazinopyridazines having antihypertensive activity having the formula: STR1 wherein R is alkyl or cycloalkyl having up to 5 carbon atoms, optionally substituted with unsubstituted phenyl, substituted phenyl or cycloalkyl, R1 is hydrogen or alkyl having 1 to 3 carbon atoms and R2 is alkyl having 1 to 3 carbon atoms, a carboxylic group or phenyl and the process for their preparation.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1291 – PubChem