Some scientific research about 2-Benzyl-4,5-dichloropyridazin-3(2H)-one

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Synthesis, in vitro/in vivo Antifungal Evaluation and Structure-Activity Relationship Study of 3(2H)-Pyridazinones

The synthesis, in vitro/in vivo antifungal evaluation and a structure-activity relationship (SAR) study of 3(2H)-pyridazinones was carried out. The results reported here may be helpful in the structural identification and understanding of the minimum structural requirements for these molecules acting as antifungal agents. In addition, the most active structure in this series was tested for its capacity of inhibiting Saccharomyces cerevisiae beta1,3-glucan synthase and chitin synthase, enzymes that catalyze the synthesis of the major polymers of the fungal cell wall.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N3211 – PubChem

 

Extracurricular laboratory:new discovery of 41933-33-9

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Synthesis of ortho-functionalized 4-aminomethylpyridazines as substrate-like semicarbazide-sensitive amine oxidase inhibitors

A series of 4-aminomethylpyridazines and -pyridazin-3(2H)-ones (“diaza-benzylamines”), bearing alkylamino side chains in ortho position relative to the CH2NH2 unit, was synthesized by catalytic hydrogenation of the corresponding nitriles in strongly acidic medium. N-Benzyl protecting groups either at the pyridazinone ring nitrogen or at an exocyclic nitrogen were selectively removed hydrogenolytically or by treatment with a Lewis acid. The new compounds were tested in vitro for semicarbazide-sensitive amine oxidase (SSAO) inhibitory activity and 4-(aminomethyl)-N,N-diethylpyridazine-3,5-diamine (22) was found to be the most active representative.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N3206 – PubChem

 

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Novel method for preparing fluorination reagent and its application to synthesis of fluoropyridazinones

4-Chloro-5-fluoro-2-aryl-3(2H)-pyridazinones were obtained by the fluorination of 4,5-dichloro-2-aryl-3(2H)-pyridazinones with ethylhexamethylenetetramine fluoride in excellent yields. The ethylhexamethylenetetramine fluoride was synthesized by the reaction of hydrofluoric acid with ethylhexamethylenetetramine hydroxide prepared from ethylhexamethylenetetramine bromide and alkali. Copyright Taylor & Francis Group, LLC.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N3216 – PubChem

 

Extended knowledge of 2-Benzyl-4,5-dichloropyridazin-3(2H)-one

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Synthesis and evaluation of nevirapine analogs to study the metabolic activation of nevirapine

Nevirapine (NVP) is widely used as a non-nucleoside reverse transcriptase inhibitor of HIV-1, however, it is associated with severe skin and liver injury. The mechanisms of these adverse reactions are not yet clear, but the metabolic activation of NVP is thought to be related to the injury process. Until now, several metabolic activation pathways of NVP have been reported. In this study, in order to identify the reactive metabolite of NVP mainly responsible for CYP inhibition and liver injury, we synthesized five NVP analogs designed to avoid the proposed bioactivation pathway and evaluated their metabolic stabilities, CYP3A4 time-dependent inhibitory activities, and cytotoxicity. As a result, only a pyrimidine analog of NVP, which could avoid the formation of a reactive epoxide intermediate, did not inhibit CYP3A4. Outside of this compound, the other synthesized compounds, which could avoid the generation of a reactive quinone-methide intermediate, inhibited CYP3A4 equal to or stronger than NVP. The pyrimidine analog of NVP did not induce cytotoxicity in HepG2 and transchromosomic HepG2 cells, expressing major four CYP enzymes and CYP oxidoreductase. These results indicated that the epoxide intermediate of NVP might play an important role in NVP-induced liver injury.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N3212 – PubChem

 

Some scientific research about 2-Benzyl-4,5-dichloropyridazin-3(2H)-one

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One-Pot Highly Regioselective Synthesis of Indole-Fused Pyridazino[4,5- b ][1,4]benzoxazepin-4(3 H)-ones by a Smiles Rearrangement

A simple and convenient synthesis of indole-fused pyridazino[4,5- b ][1,4]benzoxazepin-4(3 H)-ones is described. A range of 2-(1 H -indol-2-yl)phenols and 4,5-dichloropyridazin-3-ones are compatible with this reaction. A Smiles rearrangement is proposed as a key step in the highly regioselective construction of the products. The easy availability of the starting materials makes this an appealing method in organic synthesis.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N3207 – PubChem

 

Simple exploration of 2-Benzyl-4,5-dichloropyridazin-3(2H)-one

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3(2H)Pyridazinone, process for its preparation and anti-allergic agent containing it

A 3(2H)pyridazinone of the formula: STR1 wherein R1 is hydrogen, methyl, C3 -C6 alkenyl, C5 or C6 cycloalkyl, benzyl, phenyl, –(CH2)m CO2 R3 (wherein R3 is hydrogen or C1 -C5 alkyl, and m is an integer of from 1 to 4), –(CH2)n A (wherein A is –OH or –N(R4)2 wherein R4 is C1 -C3 alkyl, and n is an integer of from 2 to 6) or –CH2 CF3 ; R2 is chlorine or bromine; each of Y1 and Y2 which may be the same or different, is hydrogen, C1 -C5 alkyl, C2 -C8 alkenyl, halogen, –OR5 (wherein R5 is hydrogen, C1 -C8 alkyl or STR2 wherein q is an integer of from 1 to 4), –CO2 R6 (wherein R6 is hydrogen or C1 -C5 alkyl), –N(R7)2 (wherein R7 is C1 -C4 alkyl) or –SR8 (wherein R8 is C1 -C4 alkyl); and Y3 is C1 -C5 alkyl, C2 -C8 alkenyl, halogen, –OR5 (wherein R5 is as defined above), –CO2 R6 (wherein R6 is as defined above), –N(R7)2 (wherein R7 is as defined above) or –SR8 (wherein R8 is as defined above), or a pharmaceutically acceptable salt thereof.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N3195 – PubChem

 

Awesome and Easy Science Experiments about 2-Benzyl-4,5-dichloropyridazin-3(2H)-one

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Synthesis of Pyrazolo<3,4-d>pyridazines from 5-(1-Methylhydrazino)-pyridazines by Means of the Vilsmeier-Haack Reaction

Reaction of 2-substituted 5-(1-methylhydrazino)-3(2H)-pyridazinones (2a-d) with dimethylformamide-phosphorus oxychloride afforded 5-substituted 1,5-dihydro-1-methyl-4H-pyrazolo<3,4-d>pyridazin-4-ones (3a-d) in good yields.However, concurrent formation of 5-substituted 2,5-dihydro-2-(2-substituted 1-chlorovinyl)-4H-pyrazolo<3,4-d>pyridazin-4-ones (6a-c, 12, 13) (minor products) and the 1-methyl-4H-derivatives (3a-c) (major ones) was observed, when starting with the corresponding 2-substituted 5-(2-acetyl-1-methylhydrazino)-3(2H)-pyridazinones (5a-c, 9, 10) under similar conditions.A plausible mechanism for the reaction is proposed.Keywords – pyridazine; pyrazolo<3,4-d>pyridazine; Vilsmeier reagent; tri-n-butyltin chloride; sodium borohydride; stereoisomer; photoisomerization; vinyl radical

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Pyridazine – Wikipedia,
Pyridazine | C4H4N3208 – PubChem

 

Some scientific research about 41933-33-9

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An efficient and practical method for the synthesis of 1-(2,6- difluorobenzoyl)-3-(2-alkyl-3-oxopyridazin-4-yl)ureas as potential chitin synthesis inhibitors

A mild and efficient method for the synthesis of 4-amino-3(2H)- pyridazinones from their corresponding 4,5-dichloropyridazinones under microwave-assisted conditions is described. A series of novel chitin synthesis inhibitors, benzoylphenylureas containing the 3(2H)-pyridazinone, were synthesized. The biological activity of these target compounds was evaluated. Springer-Verlag 2006.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N3201 – PubChem

 

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Tri-component reaction of 2-alkyl-4,5-dichloropyridazin-3(2H)-ones: Synthesis of 5-cyano-5-(pyrimidin-2-yl)-2,7-dialkyl-5H-dipyridazino-[4,5-b:4,5- e]-4H-thiopyran-1,6-dione and 2-(4-cyanophenoxy) pyrimidine

Reaction of 2-alkyl-4,5-dichloropyridazin-3(2H)-ones with p-cyanophenol and 2-mercaptopyrimidine in the presence of base gave 2,4,5-trisubstituted- pyridazin-3(2H)-ones 4-9, 2-(4-cyanophenoxy)pyrimidine (10) and 5-cyano-5-(pyrimidin-2-yl)-2,7-dialkyl-5H-dipyridazino[4,5-b:4,5-e] -4H-thiopyran-1,6-diones 11 as a novel heterocycle.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N3215 – PubChem

 

Archives for Chemistry Experiments of 41933-33-9

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 41933-33-9, name is 2-Benzyl-4,5-dichloropyridazin-3(2H)-one, introducing its new discovery. Quality Control of 2-Benzyl-4,5-dichloropyridazin-3(2H)-one

AZABICYCLIC HETEROCYCLES AS CANNABINOIND RECEPTOR MODULATORS

The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I and Formula II: including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3 and R4 are described herein.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N3199 – PubChem