58results about How to "Wide substrate applicability" patented technology

The invention relates to the field of organic chemical synthesis, in particular to a method for stereodivergently synthesizing an iodo-allyl compound, which comprises an E-type iodo-allyl compound and a Z-type iodo-allyl compound. The invention provides a novel method for stereodivergently synthesizing the iodo-allyl compound, and the method is wide in substrate applicability and can be used for preparing various iodo-allyl compounds; meanwhile, in the presence of a photocatalyst or a manganese catalyst and alkali, the iodo-allyl compound can be prepared in a three-dimensional divergent manner only through visible light irradiation without high temperature and high pressure, that is, the reaction condition is mild, and the operation is simple; meanwhile, the method is wide in substrate applicability and can be used for preparing various iodo-allyl compounds. The specific initial raw materials are adopted, the initial raw materials do not need to be subjected to any other treatment and modification and can be directly used for the reaction, the reaction steps are few, the process is simple, and wide application prospects are achieved.

The invention relates to the field of organic synthesis, in particular to a synthesis method of gamma-aminophosphine oxide compounds and derivatives thereof. According to the synthesis method disclosed by the invention, alpha, beta-unsaturated amide, diaryl phosphine oxide or phosphite ester is taken as raw materials, and under the action of acid, the gamma-aminophosphine oxide compound can be rapidly and efficiently synthesized by a one-pot method. The preparation method comprises the following steps of: generating conjugated nitrile positive ions or imine salt intermediates with strong electrophilicity from alpha, beta-unsaturated amide under the activation of acid, converting diaryl phosphine oxide or phosphite ester into strong nucleophilic three-coordination phosphorus species under the action of alkali, and further performing phosphorus-doped Michael addition reaction on the conjugated intermediates to finally generate the gamma-aminophosphine oxide compounds. According to the method disclosed by the invention, diaryl phosphine oxide or phosphite which is cheap, easy to obtain and stable in structural property is used as a phosphorus source, the substrate applicability is wide, and the economic cost is relatively low; in addition, the method realizes synthesis of a target product without participation of a metal catalyst, and is rapid and efficient.

This invention discloses a method for the deamination functionalization of aliphatic nitrosamines, comprising: reacting an aliphatic nitrosamine as shown in formula (II) with a nucleophile in the presence of an acid and a solvent to generate a deamination functionalized product as shown in formula (III); wherein, R 1 R 2 R 3 Each group is independently selected from hydrogen, hydroxyl, alkyl, alkoxy, alkanoyl, alkoxycarbonyl, alkylsulfinyl, alkylsulfonyl, aryl, heteroaryl, phenylalkyl, or R 1 R 2 R 3 Two or three of the functional groups form a non-aromatic ring, cage-like compound; FG is a functional group in which a nucleophile participates in the reaction. The method of this invention has the advantages of inexpensive and readily available raw materials, simple reaction conditions, and wide substrate applicability.

The application belongs to the field of organic synthesis and relates to a copper-catalyzed halogen exchange method of halogenated aromatic hydrocarbons. The method is that an imine shown in the following formula is used as a ligand, and copper is used to efficiently catalyze the exchange reaction between aryl halide and a halogen source to obtain a halogen exchange product, wherein the halogen source is at least one of an iodine source, a bromine source and a chlorine source. The halogen exchange catalytic system developed by the application has wide substrate applicability, a green and mild reaction system, and the iodine source, the bromine source and the chlorine source used are cheap and easy to obtain, and the application has good industrial application value.

In the presence of an acidic reagent and an oxidizing agent, 2-indolone and indole are used as raw materials for one-step reaction to prepare the symmetric and asymmetric indole [2, 3-a] carbazole derivatives, the used raw materials, the acidic reagent and the oxidizing agent are cheap and easy to obtain, the reaction system is simple, the operation is simple, and the reaction steps are short (one-step reaction); the method has the advantages of wide substrate applicability, good functional group compatibility, mild reaction conditions, fast reaction speed, good chemical selectivity, realization of industrial production, and substantial economic and social benefits.

The application discloses a kind of dihydrotriazole aromatization precursor, preparation method and the dihydrotriazole aromatization precursor in the deacyl arylation of ketone, and the application includes: (1) ketone and 2-pyridyl hydrazine amide are dissolved in solvent, then active additive is added, and heating activation reaction is carried out under inert gas atmosphere, to obtain dihydrotriazole aromatization precursor;(2) the product of step (1) is mixed with aryl halide after or without purification, and is carried out under the conditions of photocatalyst, nickel catalyst, base, solvent and light irradiation photocatalytic reaction, to obtain the deacyl arylation product of ketone.The deacyl arylation reaction method of ketone of the application has the advantages that raw material is simple and easy to obtain, reaction condition is mild, substrate applicability is wide, etc., meets the requirements of developing green environment-friendly chemistry.

The invention relates to the field of polymer modification preparation, in particular to a preparation method of a phenoxy resin toughening agent, which comprises the following steps: carrying out epoxy group ring-opening reaction on a bisphenol diglycidyl ether compound and a polyacid compound under the action of triethylamine to obtain the phenoxy resin toughening agent, the molar ratio of the bisphenol diglycidyl ether compound to the dicarboxylic acid compound is 1: (2.0-4.0); the molar ratio of the triethylamine to the bisphenol diglycidyl ether compound is greater than or equal to 0.1; the temperature of the ring-opening reaction of the epoxy group is 55 DEG C or above. The invention further designs the phenoxy resin prepared by the preparation method and toughening application thereof. According to the method, phenoxy resin can be successfully synthesized, and the toughening effect of a bisphenol diglycidyl ether curing product can be improved.

The present invention provides a method for trans-hydroboration of a biaryl internal alkyne compound, comprising the following steps: in the presence of a nickel catalyst, a nitrogen ligand and a base, a biaryl internal alkyne compound represented by formula (I) is subjected to a trans-hydroboration reaction with bipyralidone diboric acid to obtain a compound represented by formula (II); the synthetic route is as follows: wherein R 1 and R 2 are independently selected from hydrogen, C 1 ‑C 6 Alkyl, methoxy, methylthio, halogen, nitro, cyano, trifluoromethyl, C 6 ‑C 14 Any of the aromatic groups. #imgabs0#

The invention discloses a synthesis method for preparing a fluorine-containing biphenyl compound by a one-pot method, which comprises the following steps: taking fluorine-containing bromobenzene 1A as an initial raw material, reacting with magnesium to generate fluorine-containing phenyl magnesium bromide, reacting with (RO) 3B, hydrolyzing to generate fluorine-containing aryl boric acid ester C, and carrying out coupled reaction with aryl chloride 2A to obtain a target product fluorine-containing biphenyl B; in the formula, R1 is H, F, C1-C6 alkyl and C1-C6 alkoxy; the R group is C1-C6 alkyl, and the R2 group is any one of H, F, C1-C6 alkyl, C1-C6 alkoxy, hydroxyl, nitryl, ester group and carbonyl. According to the method, fluorine-containing bromobenzene is used as a raw material, fluorine-containing phenyl magnesium bromide is prepared from fluorine-containing bromobenzene and magnesium, fluorine-containing phenyl magnesium bromide reacts with boric acid ester and is hydrolyzed to prepare fluorine-containing aryl boric acid ester, and aryl chloride is directly coupled to obtain a target product fluorine-containing biphenyl through a one-pot method without treatment; the method is simple and convenient, can be completed in one pot without post-treatment, and is high in yield and controllable in cost.

The invention discloses a preparation method for photocatalytic synthesis of an aza-aromatic compound and application of the aza-aromatic compound. The preparation method comprises the following steps: mixing an isonitrile compound, an alkyl boric acid reagent, a photosensitizer, an alkali reagent and a solvent, and reacting under the irradiation of visible light to obtain the aza-aromatic compound. The synthesis method has the advantages of easily available raw materials, simple operation, mild reaction, wide substrate applicability and the like, and the obtained indole / pyrrolo [1, 2-a] quinoxaline compound has fluorescence property.

The application discloses a preparation method of S4-(2-cyanoethyl)-4-thiothymine deoxyriboside monomer, and 5'-O-DMT-uridine is used as a starting material. First, the starting material is reacted with a sulfonylation reagent to generate a sulfonylation reaction on a carbonyl group at a 4 position of the starting material to obtain compound II. Then, the compound II is reacted with 3-mercapto propionitrile to continuously generate a substitution reaction on the 4 position to obtain compound III. Finally, the compound III is reacted with a phosphorus reagent to obtain the S4-(2-cyanoethyl)-4-thiothymine deoxyriboside monomer. The method does not need to protect a 3'-hydroxyl group, has a shorter reaction route, milder reaction conditions, and high synthesis efficiency.

The invention relates to a preparation method of a (Z)-beta-sulfonamide-alpha, beta-unsaturated carbonyl series compound, which comprises the following steps of: carrying out high-selectivity C (sp2)-H bond direct amination reaction on a compound containing alpha, beta-unsaturated carbonyl and N-fluoro diaryl sulfonamide serving as reaction substrates under the combined action of a cheap and easily available copper catalyst and alkali, thereby obtaining the (Z)-beta-sulfonamide-alpha, beta-unsaturated carbonyl series compound. (Z)-beta-sulfamido-alpha, beta-unsaturated carbonyl series compounds are prepared with high efficiency and high stereoselectivity. According to the method, the (Z)-type olefin derivative can be directionally obtained. The method has the advantages of high reaction chemical, regional and stereoselectivity, wide substrate applicability, simple reaction operation, mild reaction conditions, short reaction time, extremely low cost, simple operation and low requirements on equipment, and is suitable for large-scale preparation.

This invention discloses a method for preparing alkenyl triazole compounds. Under the action of a base, alkynyl sulfonium salts and triazole compounds are reacted in an organic solvent at room temperature and pressure for 2–5 h to obtain alkenyl triazole compounds. This invention utilizes a diamine reaction at room temperature, requiring no additional catalyst or oxidant, exhibiting excellent functional group tolerance and broad substrate applicability, while also demonstrating good chemoselectivity, regioselectivity, and stereoselectivity. The reaction system is free of toxic metal catalysts, simple to operate, and demonstrates excellent functional group tolerance and broad substrate applicability. The raw materials used are inexpensive and readily available, exhibiting good atom economy and step economy, providing a new strategy for the synthesis of triazole series compounds. The entire reaction process is mild, with high product selectivity, simple operation, and environmental friendliness, conforming to the principles of green chemistry.

The invention relates to a method for preparing gamma-amino acid derivatives and dipeptides. Specifically, under the catalytic condition of cobalt and nitrogen ligands, N-alkylamide and olefin are subjected to carbonylation to prepare gamma-amino acid derivatives and dipeptide compounds. Various amides, alcohols, phenols and amines widely existing in the industry are used as raw materials. The C3 bifunctional gamma-amino acid derivative and the dipeptide compound are obtained with high substrate compatibility and high yield under the action of a catalytic amount of cobalt catalyst by taking gas CO as a C1 source and ethylene gas as a C2 source.

The present invention belongs to the technical fields of organic synthesis, fine chemicals and pharmaceutical synthesis, and specifically relates to a method for preparing γ-vinylidene-butenoic acid lactones and / or benzofulvene compounds. The method utilizes an acid-catalyzed dehydration rearrangement reaction of cyclopropenyl alcohol derivatives to achieve the synthesis of two important compounds, γ-vinylidene-butenoic acid lactone and benzofulvene, under the condition of a "one-pot reaction"; at the same time, the preparation method is used as an important synthesis strategy to achieve the efficient synthesis of the anti-inflammatory drug rofecoxib and the benzofulvene natural product anmindenol A.

The invention discloses a method for preparing a thiophosphine (phosphorus) ester substituted benzofluorene compound, wherein the method is to use a 1,6-diynol compound as shown in formula (I) as a raw material, add an organic solvent to fully dissolve under room temperature, and then add a P(O)-SH compound, react for 1-10 hours at 80°C, and after the reaction is completed, the reaction product is separated and purified by silica gel column chromatography to obtain a thiophosphine (phosphorus) ester substituted benzofluorene compound as shown in formula (II). The raw materials of the present invention are simple and easy to obtain, the conditions are mild, the operation is simple, the substrate applicability is good, the yield is good, etc.; in addition, the prepared target product thiophosphine (phosphorus) ester substituted benzofluorene compound has potential application value in the fields of organic synthesis, pharmacy, materials science, and the like, and has a chemical synthesis method with good promotion and application prospects.

The invention discloses a method for synthesizing oxime compounds by catalyzing carbon-hydrogen bond oxidation with tetradentate nitrogen-containing coordinated manganese. With tetradentate nitrogen-containing coordinated manganese as a catalyst, under the condition of H2O2 as an oxidant, selective oxidation of carbon-hydrogen bonds of various organic compounds is achieved by adding organic carboxylic acids, and the obtained intermediate product is oximated with hydroxylamine or hydroxylamine hydrochloride or hydroxylamine sulfate, and then further alkalized to generate various ketone oxime structure products such as aromatic ketone oxime, alkyl ketone oxime, allyl ketone oxime, propargyl ketone oxime, etc. with various functional groups. Compared with the existing method, the catalytic reaction raw materials of the present invention are cheap and easy to obtain, the substrate range is wide, the catalyst dosage is small, the reaction conditions are mild, it is green and environmentally friendly, water is the only byproduct in the reaction, the selectivity is good, the yield is high, and the production cost is low.

The invention discloses a preparation method of a 2-substituted quinazoline derivative, which comprises the following step: heating and stirring three components, namely an ammonium salt, a benzyl alcohol compound and a 2, 1-benzisoxazole compound in an organic solvent to obtain the 2-substituted quinazoline derivative. According to the method, ammonium iodide which is low in price and easy to obtain is used as a nitrogen source and an oxidizing agent, benzyl alcohol is used as a carbon source, and efficient construction from a 2, 1-benzisoxazole skeleton to a 2-substituted quinazoline skeleton is achieved through a carbon-nitrogen diatom inserted ring expansion reaction under the mild conditions of no metal and no additive. The synthetic method developed by the invention has a good application prospect in the industrial fields of biological medicines, pesticides and the like, and is particularly suitable for efficiently preparing the quinazoline compound with biological activity under simple and convenient conditions. The synthetic method developed by the invention has a good application prospect in the industrial fields of biological medicines, pesticides and the like, and a theoretical basis is provided for commercialized application of the derivatives in the field of medicines.

The invention discloses a method for asymmetric catalytic synthesis of an oxygen-containing multi-element bridged ring compound, and belongs to the field of organic synthesis. According to the method, 2-hydroxycinnamaldehyde or a derivative 1 thereof and beta-nitroketone 2 are taken as raw materials, chiral secondary amine is taken as a catalyst, and reaction is performed in an organic solvent under the action of organic alkali; and after the reaction is finished, separating and purifying by silica gel column chromatography to obtain a target product 4. The synthesis of the chiral oxygen-containing multi-element bridged ring compound is completed from simple and easily available 2-hydroxycinnamyl aldehyde or a derivative thereof and nitroketone, the method has wide substrate applicability, and a new method is provided for construction of chiral heterocyclic skeletons such as multi-substituted oxygen-containing multi-element bridged rings; a new reaction path is developed, and diversified synthesis of the functional group-oriented chiral bridged ring compound is realized in one step through an addition / elimination / cyclization reaction sequence; the reaction conditions are mild, the substrate and the catalyst are easy to obtain, the reaction system is simple and clean, and the target product can be obtained with higher yield and excellent enantioselectivity.

This invention belongs to the technical field of organic synthesis and discloses a method for synthesizing 1,n-dianitronic compounds. The method involves reacting alkenyl-substituted alkyl nitriles and boric acid compounds in an air atmosphere using an organic solvent as the reaction medium, under the action of a weakly basic salt and a catalyst, to obtain 1,n-dianitronic compounds. The structure of the 1,n-dianitronic compounds is as shown in Formula I. This method utilizes readily available raw materials, offers high yield, has broad substrate applicability, is simple to operate, and boasts high atom economy, enabling the construction of structurally diverse polysubstituted 1,n-dianitronic compounds.

The invention relates to a method for preparing gamma-amide ester. Specifically, under the catalytic condition of cheap metal cobalt, formamide, phenol or alcohol and ethylene gas are subjected to carbonylation to prepare gamma-amide ester. Formamide compounds and phenol or alcohol widely existing in the nature are used as raw materials, wherein the raw materials comprise formamide, phenol and alcohol. According to the method, a formamide gamma-position carbonylation product is obtained with high atom utilization rate and high yield under the action of one or two of a catalytic amount of cheap metal agents by taking gas CO as a C1 source and ethylene gas as a C2 source.

The invention discloses a synthesis method and application of an asymmetric ether compound, and belongs to the technical field of organic synthesis. According to the method disclosed by the invention, stoichiometric silver trifluoromethanesulfonate is taken as a catalyst, benzyl halides with different structures directly react with benzyl alcohol under the conditions of air atmosphere, room temperature and no need of keeping out of light, and the asymmetric ether bond is efficiently constructed. Aromatic groups in the benzyl halide and the benzyl alcohol are independently selected from aryl or five-membered to six-membered heteroaryl containing nitrogen, oxygen and sulfur heteroatoms. The method provided by the invention is mild in condition, safe and simple to operate, wide in substrate applicability, simple in post-treatment and easy for industrial amplification, and the prepared asymmetric ether compound has very high application value in preparation of drugs and pesticides.

The invention belongs to the technical field of organic chemistry, and discloses a method for synthesizing meta-position secondary alkyl substituted aryl carboxylic acid. According to the method, in a protective atmosphere, an organic solvent is taken as a reaction medium, aryl carboxylic acid and substituted Katritzky salt react under the action of a ruthenium catalyst, a ligand, an additive and an alkaline compound, and meta-position secondary alkyl substituted aryl carboxylic acid is obtained. According to the invention, meta-position secondary alkyl substituted aryl carboxylic acid is successfully synthesized, and meta-position C-H bond secondary alkylation is realized. The method provided by the invention has the advantages of high yield, wide substrate applicability, cheap and easily-prepared raw materials, simple operation and mild conditions, and is expected to be practically applied to large-scale production.

The invention discloses a functional ionic liquid catalyst, and relates to the technical field of catalysts, the functional ionic liquid catalyst comprises cations and anions, the cations are at least one of 1, 8-diazacyclo [5, 4, 0] undecene, choline hydroxide and 1, 1, 3, 3-tetramethylguanidine, and the anions are at least one of pyrrole and 2-hydroxypyridine. The invention also discloses an application of the functional ionic liquid catalyst in catalysis of carboxylation reaction of CO2 and 2-aminobenzonitrile and derivatives thereof. The synthesis process is simple, the prepared functional ionic liquid catalyst does not contain halide components, corrosion to metal equipment can be reduced, and the service life of the equipment can be prolonged.

The invention designs a synthesis method of alpha-amino nitrile based on N, N-disubstituted amino malononitrile, and discloses that aldehyde and N, N-disubstituted amino malononitrile are taken as substrates, acetic acid is taken as an activating agent, water is taken as a solvent, the alpha-amino nitrile is obtained through reaction at 120 / 80 DEG C, the reaction condition is mild, and the alpha-amino nitrile has good functional group tolerance. The method is simple in reaction condition, wide in substrate applicability and convenient to operate, and overcomes the defects in the prior art.

The invention belongs to the field of polymer synthesis and materials, and particularly relates to an oxazolidinone polymer as well as a preparation method and application thereof. A binary alkyne monomer, a binary aldehyde monomer, carbon dioxide and monoamine are used as raw materials and react in the presence of cuprous iodide and a polar aprotic solvent to obtain the polymer, and the oxazolidinone polymer has the following structural general formula: # imgabs0 # R1, R2 and R3 are same or different organic groups. The reaction raw materials of the synthesis method are easy to obtain, the reaction condition is mild, a precious metal catalyst is not needed, and the reaction cost is reduced to a great extent. In addition, the reaction has wide substrate applicability and good functional group compatibility, and various functional groups can be introduced. The oxazolidinone polymer prepared by the invention has good processability, relatively high thermal stability and aggregation-induced emission performance, and has important application value in the aspects of optical plastics, biomedical materials, optical anti-counterfeiting, fluorescence sensing and the like.

The invention discloses a fluorescent probe for cell imaging as well as a synthesis method and application thereof. The fluorescent probe is a compound with a structure as shown in a formula (I). In the formula, R1, R2 and R3 groups are respectively and independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl; x group is O, S or NH; y group is O, S or N; the Z group is O, S or N; and the Ar group is substituted or unsubstituted aryl or heteroaryl. The fluorescent probe disclosed by the invention can be used for targeting mitochondrial fluorescence imaging, and also can be used for potential imaging of other organelles. # imgabs0 #

The invention relates to a hydroxyl selective phosphorylation protection method based on an iron catalyst and application, and the method comprises the following steps: mixing a polyhydroxy substrate, an aprotic solvent, the iron catalyst, an acid-binding agent and a phosphorylation reagent, carrying out phosphorylation reaction, and carrying out post-treatment to obtain a selective phosphorylation protection product. Under the action of the iron catalyst, the polyhydroxy substrate reacts with the phosphorylation reagent, so that one or two hydroxyl groups in the polyhydroxy substrate can be protected by phosphoryl groups with high selectivity, the efficient and high-selectivity phosphorylation process of the polyhydroxy substrate is realized, the yield of the obtained product is high, the reaction conditions are mild, and the method is suitable for industrial production. Operation is simple, convenient and efficient, and industrial production is achieved.

This invention discloses a method for synthesizing chiral quinone alcohols from phenol derivatives using chiral manganese-catalyzed oxidation. Using chiral tetradentate nitrogen-coordinated manganese as a catalyst, and under H₂O₂ oxidant conditions, the selective oxidation of various phenol derivatives to para-chiral quinone alcohols is achieved by adding organic carboxylic acids. Compared with existing methods, this invention offers advantages such as readily available and broad-ranging substrates, good functional group compatibility, low catalyst dosage, mild reaction conditions, simple operation, environmental friendliness, no waste generation, good regio and stereoselectivity, and low production cost.

The invention discloses a method for organic catalytic synthesis of a beta-amido azole compound, which comprises the following steps: in an argon atmosphere, adding a copper metal catalyst and pyridine organic small molecules into a solvent, stirring at room temperature to react for 0.5 hour, and gradually changing the color of the system from colorless to red; then, sequentially adding reaction substrates, namely fluoro-bis (benzenesulfonyl) imide, an olefin compound and an azolylation substrate into the system, and stirring and reacting at room temperature for 6 hours; and after the reaction is finished, draining the solvent to obtain a crude product, and carrying out column chromatography separation and purification on the crude product to obtain the beta-aminoazole compound. According to the invention, one-step synthesis of the beta-amido azole compound is realized, and the adopted reaction raw materials are wider, so that the substrate range of the synthesized product is further expanded.