- Synthesis method of 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone
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The invention provides a synthesis method of 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone. The method is shown in the following reaction process. The method comprises the following steps: 1) performing addition elimination on a p-chlorobenzyl halide metal reagent and cyclopropyl methyl ketone to obtain a compound as shown in a formula (II); and 2) oxidizing the compound as shown in the formula (II) to obtain a compound as shown in a formula (I), namely 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone. The method provided by the invention has the advantages of short synthetic route, high yield, low raw material cost, green and environment-friendly process, suitability for industrial large-scale production and the like.
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Paragraph 0050; 0069; 0074-0077
(2021/07/17)
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- Synthesis method of 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone
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The invention relates to a synthesis method of 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone, which comprises the following steps: 1) carrying out condensation on alpha-halogen substituted p-chlorobenzylphosphonate and cyclopropylmethyl ketone under alkaline conditions to obtain an alkenyl halide compound; and 2) hydrolyzing the alkenyl halide compound prepared in the step 1) to obtain the 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone. According to the synthetic method of 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone, alpha-halogen substituted p-chlorobenzyl phosphonate and cyclopropylmethyl ketone are condensed under the alkaline condition to obtain the alkenyl halide compound, the obtained alkenyl halide compound is hydrolyzed to obtain 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone, the whole technological process is simple and smooth, reaction conditions are mild, and the method is suitable for industrial large-scale production; alpha-halogen substituted p-chlorobenzyl phosphonate and cyclopropylmethyl ketone are used as reaction substrates, so that the method is high in atom economy, green, environment-friendly and low in raw material cost.
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Paragraph 0035; 0038-0039; 0042
(2020/02/10)
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- A 1 - (4 - chlorophenyl) -2 - cyclopropyl -1 - acetone synthetic method
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The invention discloses a 1 - (4 - chlorophenyl) - 2 - cyclopropyl - 1 - propanone synthetic method, in formula (I) of the formula (II) compound as a raw material, in the presence of a catalyst prepared by cross-coupling reaction of 1 - (4 - chlorophenyl) - 2 - cyclopropyl - 1 - propanone. The invention selective (I) of the formula (II) compound as the raw material for preparing 1 - (4 - chlorophenyl) - 2 - cyclopropyl - 1 - propanone, compared with the prior art, the reaction of the invention raw materials are easy, short synthetic route, the process is simple, after treatment is simple, the production cost is low, and the obtained 1 - (4 - chlorophenyl) - 2 - cyclopropyl - 1 - propanone high purity, in 98.5% or more, the yield and the reaction conversion is also high, the product yield is 80 - 92%.
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Paragraph 0016; 0017
(2018/10/02)
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- Preparation method of cyproconazole intermediate 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone
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The invention discloses a preparation method of cyproconazole intermediate1-(4-chlorphenyl)-2-cyclopropyl-1-acetone. Compounds in a formula (I) and a formula (II) are taken as raw materials and are subjected to a weinreb ketone synthesis reaction, and 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone is prepared. The compounds in the formula (I) and the formula (II) are taken as raw materials for preparation of 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone. Compared with the prior art, the preparation method has the advantages that reaction raw materials are easy to obtain, no catalyst is used, the synthesis route is short, the process is simple and the production cost is low; 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone has high purity reaching 98.5% or above, higher yield being 80%-88% and higher conversion rate.
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Paragraph 0014
(2018/10/19)
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- C-H functionalisation of aldehydes using light generated, non-stabilised diazo compounds in flow
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The difficulty in accessing and safely utilising non-stabilised diazo species has in the past limited the application of this class of compounds. Here we explore further the use of oxadiazolines, non-stabilised diazo precursors which are bench stable, in direct, non-catalytic, aldehyde C-H functionalisation reactions under UV photolysis in flow and free from additives. Commercially available aldehydes are coupled to afford unsymmetrical aryl-alkyl and alkyl-alkyl ketones while mild conditions and lack of transition metal catalysts allow for exceptional functional group tolerance. Examples are given on small scale and in a larger scale continuous production.
- Dingwall, Paul,Greb, Andreas,Crespin, Lorène N.S.,Labes, Ricardo,Musio, Biagia,Poh, Jian-Siang,Pasau, Patrick,Blakemore, David C.,Ley, Steven V.
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supporting information
p. 11685 - 11688
(2018/11/02)
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- Preparation method of 1-(4-chlorphenyl)-2-cyclopropyl-1-actone
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The invention provides a preparation method of 1-(4-chlorphenyl)-2-cyclopropyl-1-actone. The 1-(4-chlorphenyl)-2-cyclopropyl-1-actone is prepared by reacting a compound of a structure in Formula (II)with p-chlorobenzaldehyde. The reaction raw material is low in price and easy to obtain, and the production cost is greatly reduced; the synthetic route is short and simple in technique; the raw material preparation and synthesis of the 1-(4-chlorphenyl)-2-cyclopropyl-1-actone are free from waste water, thus the risk to people and environment is reduced; and the green and environment-friendly chemical industry development requirement is met.
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Paragraph 0029; 0061-0062
(2018/04/03)
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- One-pot synthesis of α,α-disubstituted Aryl-1-ethanones via the Wittig-Horner reaction
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A one-pot methodology for the synthesis of α,α-disubstituted aryl-1-ethanones via the Wittig-Horner reaction has been developed and described in this manuscript. Both aryl/alkyl and dialkyl α-branched arylethanone were obtained in high yields (up to 96%) without the use of any metal catalysts. A total of 14 α,α-disubstituted arylethanone derivatives were synthesized based on this simple method that easily converts the carbonyl carbon (sp2) into the sp3 carbon. This versatile method is expected to further promote the use of substituted ketones as synthetic building blocks to construct a variety of α-branched aryl ketones.
- Yang, Yunxia,Wang, Le,Chen, Yuan,Dai, Yiru,Sun, Zhihua
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p. 121 - 126
(2018/01/04)
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- Preparation method of 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone
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The invention discloses a preparation method of 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone. The method comprises the steps of preparing acetal by adopting p-chlorobenzaldehyde and phenylcarbinol or a derivative thereof as raw materials under the action of a catalyst, reacting an acetal product with trimethyl phosphite or triethyl phosphite in an environment of a polar solvent under the catalysis of lewis acid to generate alpha-benzyloxy p-chlorobenzyl dimethyl phosphate, further reacting the alpha-benzyloxy p-chlorobenzyl dimethyl phosphate with cyclopropyl methyl ketone under the combined action of a base catalyst, a phase transfer catalyst and a cocatalyst to prepare a benzyloxy-propylene derivative; and then carrying out acidifying hydrolysis on the benzyloxy-propylene derivative to obtain the1-(4-chlorphenyl)-2-cyclopropyl-1-acetone. Compared with the prior art, the method has the advantages of being safe in operation, controllable in process, low in toxicity in the process, mild in reaction condition, suitable for industrial production and high in product purity.
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- A 1 - (4 - chlorophenyl) - 2 - cyclopropyl - 1 - propanone synthetic method
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The invention relates to a synthetic method of 1-(4-chlorophenyl)-2-cyclopropyl-1-propanone. The synthetic method comprises steps as follows: (1), hydroxy lamine hydrochloride is dissolved in a solvent, alkali is added, the pH (potential of hydrogen) value is adjusted, a raw material of cyclopropyl propionaldehyde is added at the appropriate temperature for a reaction, and cyclopropyl acetaldoxime is obtained through extraction, concentration and drying after the reaction ends; (2), newly prepared p-chlorophenyl diazonium salt and a catalyst are added to cyclopropyl acetaldoxime at the lower temperature, acid is added, the mixture is heated to have a reaction, and 1-(4-chlorophenyl)-2-cyclopropyl-1-propanone is obtained through aftertreatment after the reaction ends. The synthetic route is shown in the specification. The synthetic method has the advantages as follows: the cost of raw materials is low, the overall yield of the reaction is high, the technological operation is safe, aftertreatment is simple and convenient, and the synthetic method has industrial application value.
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Paragraph 0038; 0039; 0040; 0041; 0042; 0043; 0044-0049
(2017/08/25)
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- Preparation method of 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone
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The invention relates to a preparation method of 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone. A compound I and cyclopropyl methyl ketone react at 0-30 DEG C to obtain a compound II under the existence of alkali and organic solvent; the compound II is hydrolyzed under the existence of acid to obtain a compound III, namely 1-(4-chlorphenyl)-2-cyclopropyl-1-acetone. The structural formulas of the compound I, the compound II and the compound III are shown in the description, R1 is any one of trimethylsilyl, acetyl and methyl sulphonyl, and R2 is methyl or ethyl. The method is simple in process, low in cost, little in three wastes, high in target product content and yield and suitable for industrial production.
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Paragraph 0026; 0028; 0029; 0036; 0038
(2017/08/27)
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- A 1 - (4 - chlorophenyl) - 2 - cyclopropyl - 1 - propanone preparation method
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The invention relates to a 1-(4-chlorophenyl)-2-cyclopropyl-1-propanone preparation method. The preparation method comprises that chlorobenzyl alcohol, sodium nitrite, acetic acid and concentrated hydrochloric acid undergo a reaction, the reaction product is treated to form a compound I, the compound I and cyclopropyl methyl ketone undergo a condensation reaction in the presence of an alkali and a solvent, the reaction product is treated to form a compound II, the compound II undergoes a reduction reaction in the presence of a reducer and a solvent, the reaction product is treated to form a compound III, the compound III undergoes a reduction reaction in the presence of a reducer and a solvent, and the reaction product is treated to form 1-(4-chlorophenyl)-2-cyclopropyl-1-propanone. The preparation method has the advantages of simple processes, use of cheap and easily available raw materials, low cost, less three wastes, industrial production feasibility and high product yield and content.
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- Preparation method of 1-(4-chlorphenyl)-2-cyclopropyl-1-cetone and intermediate thereof
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The invention relates to a preparation method of 1-(4-chlorphenyl)-2-cyclopropyl-1-cetone. The preparation method comprises the following steps: by using alpha-hydroxy p-chlorobenzyl phosphonate shown in a formula I and 3,4-2H-dihydropyran as raw materials, preparing under the condition of existence of a catalyst, so as to obtain a compound shown in a formula II; reacting the compound shown in the formula II and cyclopropyl methyl ketone under the condition of existence of alkaline and a solvent, so as to obtain a compound shown in a formula III; enabling the compound in the formula III to generate hydrolysis reaction under the acid condition, so as to obtain the 1-(4-chlorphenyl)-2-cyclopropyl-1-cetone. The preparation method of the 1-(4-chlorphenyl)-2-cyclopropyl-1-cetone has the advantages that the alpha-hydroxy p-chlorobenzyl phosphonate shown in the formula I and the 3,4-2H-dihydropyran are used as the raw materials, the prices of the raw materials are low, the obtaining is easy, the steps are simple, the cost is low, the three-waste pollution is little, the green and environment-friendly effects are realized, and the preparation method is suitable for industrialized production; the purity of the prepared 1-(4-chlorphenyl)-2-cyclopropyl-1-cetone is high, the content is 96% or more, and the yield is high and is 83% or more.
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Paragraph 0063; 0067; 0068; 0069; 0071
(2017/07/19)
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- A 1 - (4 - chlorophenyl) - 2 - cyclopropyl - 1 - propanone synthetic method (by machine translation)
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The invention relates to a 1 - (4 - chlorophenyl) - 2 - cyclopropyl - 1 - propanone synthetic method, the synthetic method specific steps are as follows: (1) will be Pcad dissolved in organic solvent, then adding phosphorous acid dialkyl ester, and under a certain temperature for a period of time alkali catalytic reaction; (2) to be after the end of the catalytic reaction, continue adding alkali, and within certain temperature range instillment cyclopropane ketone, reaction after a period of time, post-treatment, distillation, relatively high-purity 1 - (4 - chlorophenyl) - 2 - cyclopropyl - 1 - propanone; reaction equation is as follows: . The advantage of this invention is characterized in that: the invention short reaction steps, equipment utilization is high, less solvent consumption, low production cost, safety and environmental protection, and the operation is convenient, post-processing mode is simple, simple purification, by distillation to obtain the content of 97% or more of the 1 - (4 - chlorophenyl) - 2 - cyclopropyl - 1 - propanone. (by machine translation)
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Paragraph 0019
(2017/05/23)
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- Preparation method of cyproconazole
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The invention relates to a preparation method of cyproconazole as shown in the chemical structural formula I. According to the preparation method, 4-chlorobenzaldehyde is selected as a raw material to undergo a Grignard reaction to obtain a key intermediate 1-(4-chlorophenyl)-2-cyclopropyl-1-propanol; and 1-(4-chlorophenyl)-2-cyclopropyl-1-propanol undergoes an oxidation reaction, and then Sulfur ylide reaction and ring-opening reaction are successively carried out to prepare cyproconazole. Preparation reaction is as shown in the specification, wherein an oxidizing agent is selected from N-halosuccinimide, 1,3-dihalo-5,5-dimethyl hydantoin or ketone-alkoxy-aluminium; a sulfur ylide reagent is prepared by carrying out a reaction between (CH3)2S and (CH3)2SO4 under the action of KOH in isobutanol; DBU is 1,8-diazabicyalo[5.4.0]C11-7-en; and NMP is N-methylpyrrolidine.
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Paragraph 0063-0066
(2017/04/08)
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- A 1 - (4-chlorophenyl) - 2-cyclopropyl-1-propanone synthesis method (by machine translation)
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The invention relates to a 1? (4? Chlorolphenyl)? 2? Cyclopropyl? 1? Method for the synthesis of acetone, 4? Paradichlorbenzene acetonitrile, cyclopropyl methyl ketone, strong alkali and phase-transfer catalyst reaction in the solvent, then the solvent in the presence of a catalyst in the final reduction of the powdered magnesium and the alkali in the presence of phase-transfer catalyst into the oxygen or air oxidation process is performed on, prepare the 1? (4? Chlorolphenyl)? 2? Cyclopropyl? 1? Acetone. Compared with the prior art, by introducing the catalyst of the present invention, reduce the reaction temperature, the elimination of the tar, improves the yield and purity, the cost is reduced, further reducing the generation of impurities, the environmental pressure is small, less occupied equipment, preparation process is simple, the operation is simple, mild condition, high yield, is suitable for large-scale industrial production. (by machine translation)
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Paragraph 0035
(2017/04/03)
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- Synthetic method of cyproconazole intermediate
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The invention relates to a synthetic method of cyproconazole intermediate. The synthetic route is as follow (see the formula in the description). The method includes the steps that p-chlorobenzaldehyde is used as a raw material, an acetal intermediate is obtained through condensation of p-chlorobenzaldehyde and ethylene glycol monomethyl ether, by means of triethyl phosphite, the acetal intermediate reacts with cyclopropyl methyl ketone under the alkaline condition, and finally the target compound (I) is obtained through hydrolysis. The synthetic method has the advantages of being safe, convenient, smooth in process and suitable for industrial production.
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- METHOD FOR PREPARING 1-(4-CHLOROPHENYL)-2-CYCLOPROPYL-1-PROPANONE AND INTERMEDIATE THEREOF
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A method is for preparing 1-(4-chlorophenyl)-2-cyclopropyl-1-propanone and an intermediate thereof, where in the method for preparing a compound of formula (I), α-alkoxy p-chlorobenzyl phosphonate (II) and cyclopropyl methyl ketone are used as raw materials, and subjected to a Homer-Wadsworth-Emmons reaction in an organic solvent in the presence of a base, so as to prepare a derivative of alkoxy propylene with the structure of formula (III); and the resulting derivative of alkoxy propylene (III) is hydrolyzed under acidic conditions to obtain 1-(4-chlorophenyl)-2-cyclopropyl-1-propanone (I).
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Paragraph 0032; 0033
(2015/11/18)
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- ANTIFUNGAL 1,2,4-TRIAZOLYL DERIVATIVES HAVING A 5- SULFUR SUBSTITUENT
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The present invention relates to novel triazole compounds of the formulae (I) and (Il) as defined below, to agricultural and pharmaceutical compositions containing them and to their use as fungicides antiviral and anticancer agents.
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Page/Page column 120
(2010/12/29)
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- Cyclopropane derivatives
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The invention provides a process for the preparation of a compound of the general formula (I): STR1 wherein X, Y and R1 to R7 are as defined. In the process, the olefinic analog of the compound of general formula (I) is treated with a halogen-bearing compound in the presence of metallic zinc.
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