70682-09-6Relevant academic research and scientific papers
Method for synthesizing 2-hylogen-3-alkyl substituted sulfonyl pyridine and midbody thereof in ultrasonic method
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Paragraph 0077; 0078; 0079; 0080; 0081, (2017/07/19)
The invention discloses a method for synthesizing 2-hylogen-3-alkyl substituted sulfonyl pyridine and midbody thereof in an ultrasonic method. The method comprises the following steps: enabling substituted amino acraldehyde, a catalyst and substituted cyanoethyl sulfone to react under ultrasonic until the complete reaction to prepare a reaction solution of a 2-hylogen-3-alkyl substituted sulfonyl pyridine midbody; adding halogen hydride into the reaction solution at a certain of temperature, facilitating the continuous reaction until the complete reaction, adding an alkaline solution into the reaction solution, adjusting a pH value to 7 to 8, standing, layering into a water layer and an organic layer, extracting the water layer by using an organic solvent, combining the organic layer, refining to obtain the 2-hylogen-3-alkyl substituted sulfonyl pyridine. The 2-hylogen-3-alkyl substituted sulfonyl pyridine is synthesized by adopting the ultrasonic method, so that the organic synthetic reaction can be effectively facilitated, the reaction speed is increased, the reaction yield is increased, and the environmental protection is facilitated; and the reaction time is short, the operation is simple, the reaction can be completed generally in two hours, the product yield is high, the quality is good, and the yield can reach 90 percent or more which is higher than the yield of the traditional solvent-method heating refluxing method.
Method for synthesizing 2-halo-3-substituted alkyl sulfonyl pyridine and intermediate thereof by using ionic liquid method
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Paragraph 0094; 0095; 0096; 0097; 0098, (2017/08/29)
The invention discloses a method for synthesizing 2-halo-3-substituted alkyl sulfonyl pyridine and an intermediate thereof by using an ionic liquid method. The method comprises the following steps: adding substituted amino acraldehyde, an ionic liquid and substituted cyanoethyl sulphone into a reactor, uniformly mixing, performing reaction, and tracking the reaction till the substituted amino acraldehyde or the substituted cyanoethyl sulphone is completely reacted so as to obtain an intermediate; adding halogen hydride into a reaction liquid for continuous reaction, and tracking detection till the reaction is completed; adding an alkali liquid into the reaction liquid to adjust the pH value to 7-8, leaving to stand and layer so as to obtain a water layer and an organic layer, extracting the water layer by using an organic solvent, combining the organic layer, and refining, thereby obtaining the 2-halo-3-substituted alkyl sulfonyl pyridine. The method for synthesizing the 2-halo-3-substituted alkyl sulfonyl pyridine, which is disclosed by the invention, has the advantages of being green and environment-friendly, short in reaction time, simple to operate, high in product yield and relatively good in bactericidal activity of products.
Method for synthesizing 2-halo-3-substited alkylsulfonyl pyridine and intermediate compound thereof through microwave method
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Paragraph 0018; 0090; 0091; 0092; 0093; 0094; 0095, (2017/07/15)
The invention discloses a method for synthesizing 2-halo-3-substited alkylsulfonyl pyridine and an intermediate compound thereof through a microwave method. The method comprises the following steps: adding substituted amino acraldehyde, a catalyst and substituent cyanoethyl sulfone into a reactor, reacting under microwave radiation, and tracking the reaction until the substituted amino acraldehyde or the substituent cyanoethyl sulfone reacts completely, thereby preparing the intermediate compound; adding halogen hydride into the reaction solution, further reacting, and tracking detection until the reaction is complete; and adding an alkaline solution into the reaction solution to regulate the pH value to 7-8, standing for stratification to obtain a water layer and an organic layer, extracting the water layer with organic solvent, then merging the organic layers, and refining to prepare the 2-halo-3-substited alkylsulfonyl pyridine. According to the invention, the method for synthesizing 2-halo-3-substited alkylsulfonyl pyridine has the advantages of greenness, environment friendliness, short reaction time, simple operation process and high product yield; and the product has favorable bactericidal activity.
Sulfonyl pyridine derivative and synthetic method thereof
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Paragraph 0054; 0055, (2017/07/22)
The invention discloses a sulfonyl pyridine derivative and a synthetic method thereof. Substituted aminoacrolein, emulsifiers and substituent cyanoethyl sulfone are added into a reactor and are subjected to reaction at a certain temperature; the reaction is tracked until the substituted aminoacrolein or the substituent cyanoethyl sulfone is disappeared; then halogen hydride is added into reaction liquid to continuously carry out reaction, and the detection is tracked until the reaction is completely carried out; alkali liquid is added into the reaction liquid to regulate the pH value to 7-8, and standing and layering treatment is carried out to obtain a water layer and an organic layer; the water layer is extracted by using an organic solvent, then the organic layer is combined, and refining is carried out to obtain the sulfonyl pyridine derivative. The problems that the synthetic reaction time of the conventional sulfonyl pyridine derivative is long and more three-wastes are produced so as to be difficultly treated are solved, and the effects that the reaction yield is so high to reach 82% or above, even being up to 93.5%, and the operation process is simple, the sulfonyl pyridine derivative is green and environment-friendly, fewer three wastes are produced, and the sulfonyl pyridine derivative is suitable for industrial production are achieved.
A water phase synthesis of 2 - halo - 3 - substituted hydrocarbyl sulfonyl pyridine and its intermediate method (by machine translation)
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Paragraph 0069; 0070, (2017/07/19)
The invention discloses a technique of synthesizing 2 - halo - 3 - substituted hydrocarbyl sulfonyl pyridine and intermediate method, substituted amino acrolein, catalyst and replace the cyanide sulfatoethyl, reaction at certain temperature, the tracking reaction to substituted amino acrolein or substituted cyanide b sulfone disappear, make the 2 - halo - 3 - substituted hydrocarbyl sulfonyl pyridine intermediates of the reaction solution; then adding hydrogen to the reaction solution to continue the reaction, tracking detection to the reaction is complete, to the reaction solution to adjust the pH value of the addition of alkali to the 7 - 8, to obtain the layered layer and the organic layer, the aqueous layer extracted by an organic solvent, then the combined organic layer, through the refining, make the 2 - halo - 3 - substituted hydrocarbyl sulfonyl pyridine. The aqueous synthesis of 2 - halo - 3 - substituted hydrocarbyl sulfonyl pyridine, effectively reduce the use of an organic solvent, in favor of environmental protection; short reaction time and the operation is simple, usually 4h can be completed within a reaction, the product yield is high, the yield can be 90% or more, higher than the traditional solvent the yield of heating reflux. (by machine translation)
HETEROARYLSULFONYL STILBENES AS 5-HT2A ANTAGONISTS
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Page/Page column 27, (2008/06/13)
Compounds of formula I: are potent and selective antagonists of the 5-HT2A receptor, and hence are useful in treatment of various 10 CNS disorders.
The Reaction of Some Halogenated Pyridine Thioethers and Sulphones with Carbon Disulphide
Dunn, A. D.,Norrie, R.
, p. 269 - 272 (2007/10/02)
Dithiocarboxylation of some halogenated pyridine sulphones with carbon disulphide and sodium hydride leads to the formation of thiomethyl derivatives via Smiles rearrangement of the initially produced dianion, fragmentation and subsequent methylation.In one instance the pyridino-1,4-dithiine 7 was obtained.The thioether 2d was also converted into a thiomethyl derivative when subjected to the same reaction sequence.
