New explortion of 2-(Methylsulfonyl)-10H-phenothiazine

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MODIFIED SYNTHESES OF 2-(METHYLTHIO)-10-(2-(1-METHYL-2-PIPERIDINYL)ETHYL)PHENOTHIAZINE (THIORIDAZINE) AND 1-(3-(2-(METHYLSULFONYL)-10-PHENOTHIAZINYL)PROPYL)-PIPERIDINE-4-CARBOXAMIDE (METOPIMAZINE)

Modified syntheses

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Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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A 2 – (methyl sulfonyl) – 10H-phenothiazine preparation method (by machine translation)

A 2 the […] (methyl sulfonyl) – 10H the method for preparing phenothiazine […], which belongs to the technical field of pharmaceutical intermediates. The method to the chlorobenzene sulfonyl chloride and 2 the sodium salt of thiophenols […] as the starting material, which has not been reported to the two novel intermediate product M1 and M3, each experimental step are different from the explore the ideal correlation reference the literature, in particular for synthesizing final product the 2 […] (methyl sulfonyl) – 10H the phenothiazine […] the cyclization process in the literature is completely breaks the restrictions of various conditions. The whole process of the method of the invention of simple steps, the operation is simple, and is easy to control the reaction mild condition, each step the advantages of the high product yield, is suitable for industrial production, the invention has the advantages of the use of the relatively large value and social and economic benefits. (by machine translation)

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Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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Preparation method of meixamethoxam intermediate (by machine translation)

Uses o-dichlorobenzene or o-difluorobenzene. to generate :(1)-amino – 4 4-methylsulfonylbenzenethiol 2 – in a hydrogenation reduction reaction 2 – The method comprises the following steps ;(2): 2 – nitro – 4 4-methylsulfonylphenylthiophenol- and o-dichlorobenzene. or o-difluorobenzene are used as the catalyst C – N/C – S in a hydrogenation reduction reaction as the ligand 2 – in the following step . The preparation method comprises the following steps: synthesizing, methylsulfonyl – 101010H-phenothiazine (2) through hydrogenation reduction . N,N,N ?, N ? -step. is, carried out through a hydrogenation reduction reaction, with an iron salt serving as a catalyst. base, in the following, steps: No.No. STR8No.No.No.No. STR8No.No.No.No. STR8No.No.No.No. STR8No.No.No. (by machine translation)

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Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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A new process for preparing us holds third paipai qin (by machine translation)

The present invention discloses a new process for preparing us holds third paipai qin, in the reactor, in order to […] thiophenol and O-nitro-P-methylsulfonyl chlorobenzene as raw materials, in acetone to obtain the 2 – (2 – fluorophenyl-thio) – 5 – (methyl sulfonyl) nitrobenzene; then adding ethanol, iron trichloride heating reaction, generating 2 – (2 – fluorophenyl-thio) – 5 – (methyl sulfonyl) aniline; then adding dimethyl sulfoxide, adding NaH, temperature reaction, adding water to the room temperature, to obtain the 2 – methylsulfonyl – 10 H – phenothiazine; along with add-on 10 – acetyl – 2 – armor asia sulphone base – 10 H phenothiazine, potassium hydroxide reaction 10 – acetyl – 2 – methyl-sulfonyl – (5 – sulfoxide) – 10 H phenothiazine; and then adding acetone, by concentrating the extraction, to obtain 10 – acetyl – 2 – methyl-sulfonyl – 10 H phenothiazine of the dichloromethane solution, the temperature of the post-piperidine – 4 – carboxamide, vinegar acid sodium borohydride, reacting filtering, the filter cake slurry to be-US […]; the invention by optimizing the reaction route and the reaction conditions, such that the final yield greatly improved, product purity is up to 99.3% or more. (by machine translation)

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Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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Synthesis and biological properties of aryl methyl sulfones

A novel group of aryl methyl sulfones based on nonsteroidal anti-inflammatory compounds exhibiting a methyl sulfone instead of the acetic or propionic acid group was designed, synthesized and evaluated in vitro for inhibition against the human cyclooxygenase of COX-1 and COX-2 isoenzymes and in vivo for anti-inflammatory activity using the carrageenan induced rat paw edema model in rats. Also, in vitro chemosensitivity and in vivo analgesic and intestinal side effects were determined for defining the therapeutic and safety profile. Molecular modeling assisted the design of compounds and the interpretation of the experimental results. Biological assay results showed that methyl sulfone compounds 2 and 7 were the most potent COX inhibitors of this series and best than the corresponding carboxylic acids (methyl sulfone 2: IC50 COX-1 = 0.04 and COX-2 = 0.10 muM, and naproxen: IC50 COX-1 = 11.3 and COX-2 = 3.36 muM). Interestingly, the inhibitory activity of compound 2 represents a significant improvement compared to that of the parent carboxylic compound, naproxen. Further support to the results were gained by the docking studies which suggested the ability of compound 2 and 7 to bind into COX enzyme with low binding free energies. The improvement of the activity of some sulfones compared to the carboxylic analogues would be performed through a change of the binding mode or mechanism compared to the standard binding mode displayed by ibuprofen, as disclosed by molecular modeling studies. So, this study paves the way for further attention in investigating the participation of these new compounds in the pain inhibitory mechanisms. The most promising compounds 2 and 7 possess a therapeutical profile that enables their chemical scaffolds to be utilized for development of new NSAIDs.

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Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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A 2 – (methyl sulfonyl) – 10H-phenothiazine preparation method (by machine translation)

A 2 the […] (methyl sulfonyl) – 10H the method for preparing phenothiazine […], which belongs to the technical field of pharmaceutical intermediates. The method to the chlorobenzene sulfonyl chloride and 2 the sodium salt of thiophenols […] as the starting material, which has not been reported to the two novel intermediate product M1 and M3, each experimental step are different from the explore the ideal correlation reference the literature, in particular for synthesizing final product the 2 […] (methyl sulfonyl) – 10H the phenothiazine […] the cyclization process in the literature is completely breaks the restrictions of various conditions. The whole process of the method of the invention of simple steps, the operation is simple, and is easy to control the reaction mild condition, each step the advantages of the high product yield, is suitable for industrial production, the invention has the advantages of the use of the relatively large value and social and economic benefits. (by machine translation)

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Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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A new process for preparing us holds third paipai qin (by machine translation)

The present invention discloses a new process for preparing us holds third paipai qin, in the reactor, in order to […] thiophenol and O-nitro-P-methylsulfonyl chlorobenzene as raw materials, in acetone to obtain the 2 – (2 – fluorophenyl-thio) – 5 – (methyl sulfonyl) nitrobenzene; then adding ethanol, iron trichloride heating reaction, generating 2 – (2 – fluorophenyl-thio) – 5 – (methyl sulfonyl) aniline; then adding dimethyl sulfoxide, adding NaH, temperature reaction, adding water to the room temperature, to obtain the 2 – methylsulfonyl – 10 H – phenothiazine; along with add-on 10 – acetyl – 2 – armor asia sulphone base – 10 H phenothiazine, potassium hydroxide reaction 10 – acetyl – 2 – methyl-sulfonyl – (5 – sulfoxide) – 10 H phenothiazine; and then adding acetone, by concentrating the extraction, to obtain 10 – acetyl – 2 – methyl-sulfonyl – 10 H phenothiazine of the dichloromethane solution, the temperature of the post-piperidine – 4 – carboxamide, vinegar acid sodium borohydride, reacting filtering, the filter cake slurry to be-US […]; the invention by optimizing the reaction route and the reaction conditions, such that the final yield greatly improved, product purity is up to 99.3% or more. (by machine translation)

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Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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MODIFIED SYNTHESES OF 2-(METHYLTHIO)-10-(2-(1-METHYL-2-PIPERIDINYL)ETHYL)PHENOTHIAZINE (THIORIDAZINE) AND 1-(3-(2-(METHYLSULFONYL)-10-PHENOTHIAZINYL)PROPYL)-PIPERIDINE-4-CARBOXAMIDE (METOPIMAZINE)

Modified syntheses

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Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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Preparation method of meixamethoxam intermediate (by machine translation)

Uses o-dichlorobenzene or o-difluorobenzene. to generate :(1)-amino – 4 4-methylsulfonylbenzenethiol 2 – in a hydrogenation reduction reaction 2 – The method comprises the following steps ;(2): 2 – nitro – 4 4-methylsulfonylphenylthiophenol- and o-dichlorobenzene. or o-difluorobenzene are used as the catalyst C – N/C – S in a hydrogenation reduction reaction as the ligand 2 – in the following step . The preparation method comprises the following steps: synthesizing, methylsulfonyl – 101010H-phenothiazine (2) through hydrogenation reduction . N,N,N ?, N ? -step. is, carried out through a hydrogenation reduction reaction, with an iron salt serving as a catalyst. base, in the following, steps: No.No. STR8No.No.No.No. STR8No.No.No.No. STR8No.No.No.No. STR8No.No.No. (by machine translation)

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Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

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Application of 23503-68-6, 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 a type is Article, 23503-68-6, molecular formula is C13H11NO2S2, introducing its new discovery.

Synthesis and biological properties of aryl methyl sulfones

A novel group of aryl methyl sulfones based on nonsteroidal anti-inflammatory compounds exhibiting a methyl sulfone instead of the acetic or propionic acid group was designed, synthesized and evaluated in vitro for inhibition against the human cyclooxygenase of COX-1 and COX-2 isoenzymes and in vivo for anti-inflammatory activity using the carrageenan induced rat paw edema model in rats. Also, in vitro chemosensitivity and in vivo analgesic and intestinal side effects were determined for defining the therapeutic and safety profile. Molecular modeling assisted the design of compounds and the interpretation of the experimental results. Biological assay results showed that methyl sulfone compounds 2 and 7 were the most potent COX inhibitors of this series and best than the corresponding carboxylic acids (methyl sulfone 2: IC50 COX-1 = 0.04 and COX-2 = 0.10 muM, and naproxen: IC50 COX-1 = 11.3 and COX-2 = 3.36 muM). Interestingly, the inhibitory activity of compound 2 represents a significant improvement compared to that of the parent carboxylic compound, naproxen. Further support to the results were gained by the docking studies which suggested the ability of compound 2 and 7 to bind into COX enzyme with low binding free energies. The improvement of the activity of some sulfones compared to the carboxylic analogues would be performed through a change of the binding mode or mechanism compared to the standard binding mode displayed by ibuprofen, as disclosed by molecular modeling studies. So, this study paves the way for further attention in investigating the participation of these new compounds in the pain inhibitory mechanisms. The most promising compounds 2 and 7 possess a therapeutical profile that enables their chemical scaffolds to be utilized for development of new NSAIDs.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem