40results about How to "Reaction economy" patented technology

The invention relates to a method for easily preparing aryl morpholine (formula I) and aryl piperidine (formula II). The preparation method mainly comprises the following steps of: reacting morpholine (formula III) or piperidine (formula IV) with aryl bromide (formula V) in an organic solvent in the presence of a catalytic amount of palladium compound with a simple structure, a phosphorus (phosphonium) ligand with a simple structure and an alkali at a certain temperature for 3-10 hours; and performing column chromatography isolation to obtain aryl morpholine (formula I) or aryl piperidine (formula II). Compared with the conventional method for preparing aryl morpholine and aryl piperidine, the method has the advantages of easiness, readily-available catalysts and ligands, low preparation cost, high yield and the like.

The invention discloses a method for preparing 1,4-dicarbonyl derivatives. Specifically, styrene derivatives and bromine-containing compounds are used as reactants, metal cobalt compounds are used as catalysts, and tert-butanol hydroperoxide is used as oxidants. 1,4-dicarbonyl derivatives were prepared by oxidative coupling reaction of alkenes in organic solvents. The preparation method disclosed by the invention has mild reaction conditions, only needs to be carried out in air, the reaction process and post-treatment are simple, and the final product can be obtained by simple column chromatography after the reaction is completed; and the raw materials used in the reaction have a wide range of sources, which is in line with the development of contemporary green chemistry requirements and directions, and has industrial application value.

The invention discloses a method for preparing oxalate: using diazo compounds and α-Br ketones as reaction substrates, and using O 2 As oxygen source and oxidizing agent, visible light is used as energy source, organic dye is used as photocatalyst, and oxalate is obtained through free radical process in organic solvent. The method used in the present invention has the following characteristics: the reaction is more environmentally friendly and economical, the substrate has wider applicability, the later functional group is easier, the reaction condition is mild, it can be carried out in the air, the amount of photocatalyst is less, and the post-treatment is simple. At the same time, the reactants, photocatalysts and other raw materials used in the present invention are cheap and easy to obtain, the reaction composition is reasonable, no ligand is needed, the atom economy is high, the reaction steps are few, and a higher yield can be obtained with only one step of reaction, which is in line with contemporary green The requirements and direction of chemistry and sustainable development are suitable for the synthesis of asymmetrically substituted oxalates that are difficult to synthesize by traditional methods.

The invention discloses a preparation method of an E-vinyl sulfones compound. The preparation method comprises the following steps: dissolving raw materials of olefin and thiophenol (thioalcohol) into a tetrahydrofuran solvent; then adding lodine pentaoxide and organic base DBU (1,8-diazabicyclo undec-7-ene); directly reacting for 12 to 16 hours under 60 to 80 DEG C; separating and purifying a coarse product after stopping reacting, thus obtaining the E-vinyl sulfones compound. The preparation method has the advantages that raw materials are simple and can be easily obtained, the price is cheap, the reaction requires no metal catalyst, metal pollution is avoided, the operation is simple and is free of harsh conditions of water free, oxygen free and the like, the adaptive range of a substrate is wide, the reaction stereoselectivity is high, the process conditions are stable, and a prepared product is easy to purify.

The invention discloses a method for preparing 1,4-dihydrooxazine. An acyl diazo derivative and an acridine compound are taken as reaction substrates, AgOTf and Cu(OAc)2 are taken as reaction catalysts, NaHCO3 is used as an alkali, and the 1,4-dihydrooxazine is obtained through a ring addition reaction in an organic solvent. The method provided by the invention has the following characteristics that the reaction is more economical, functionalization in the later period is easier, reaction conditions are mild, the reaction can be carried out in the air, the use amount of the catalysts is small,post-treatment is simple and convenient, purification and large-scale industrial application of the product are facilitated, and one-step functionalization of commercial medicines is easier to carryout. Meanwhile, the raw materials such as the reactants, the catalysts and the like are cheap and easily available, the reaction composition is reasonable, a ligand is not needed, the atom economy ishigh, the reaction steps are few, and a relatively high yield can be obtained only by the one-step reaction, so that the method accords with requirements and directions of contemporary green chemistryand pharmaceutical chemistry and is suitable for screening high-activity 1,4-dihydrooxazine medicines, a gram-grade reaction can be well realized, and the method is suitable for large-scale industrial production.

The invention discloses a method for preparing polysubstituted pyrazoles, and develops a new catalytic system for aryl diazonium salts, using alkynoate and diazo ester derivatives as reaction substrates, using toluene as solvent, through cyclization / N ‑H insertion reaction to prepare polysubstituted pyrazoles. The method used in the present invention has the following characteristics: economical reaction, wider substrate universality, mild reaction conditions, can be carried out in the air, less catalyst consumption, convenient post-treatment, and is beneficial to product purification and industrial application. At the same time, the raw materials such as reactants and catalysts used in the present invention are cheap and easy to obtain, the reaction composition is reasonable, no ligand is needed, the reaction steps are few, and only one step reaction can achieve excellent yield, which meets the requirements and requirements of contemporary green chemistry and medicinal chemistry. direction.

The invention discloses a method for preparing amino-acid ester. In the presence of an oxidant, the method adopts an amine compound and malonic ester as reactants, an iodide as a catalyst and sodium acetate as alkali; a product amino-acid ester is prepared through nucleophilic substitution in a polar solvent; the general formula of the chemical structure of malonic ester is shown in the decstiption; and the iodide is one of I2, TBAI, NIS and IBr. According to the method disclosed by the invention, the reaction activity of the catalyst is high, the reaction conditions are moderate, the application range of substrate is wide, the aftertreatment is convenient, the yield of the target product is high, the preparation process is simple and green and environment-friendly, and the raw materials are widely available.

The invention discloses a method for preparing α-cyanoamine. In the presence of an oxidizing agent, an amine compound and cyanoacetic acid are used as reactants, iodide is used as a catalyst, and sodium acetate is used as a base. The nuclear substitution reaction prepares the product α-cyanoamine. The method of the invention has high catalyst reactivity, mild reaction conditions, wide application range of substrates, convenient post-treatment, high yield of target product, simple preparation process, green and environmental protection, and wide sources of raw materials used.

The invention relates to a method for synthesizing acrylic alkoxy ethyl ester or methacrylic acid alkoxy ethyl ester. Under the action of SO4<2-> / TiO2 solid super acidic catalyst, phenothiazine inhibitor, phenothiazine-hydroquinone-copper powder composite inhibitor or toluene azeotropic dehydrating agent, acrylic acid or methacrylic acid and glycol monoalkyl ether are taken as raw materials and are directly esterified to acrylic alkoxy ethyl ester or methacrylic acid alkoxy ethyl ester. A preparation method of the solid super acidic catalyst SO4<2-> / TiO2 comprises the following steps that: reacting TiCl4 with ammonia water; aging precipitate, filtering, washing till no Cl<-> and drying to obtain a carrier TiO2; dipping the TiO2 carrier in H2SO4 with the concentration between 0.25 and 1.0 mol / L, washing, drying and calcining for 3 to 5 hours at a temperature between 400 and 600 DEG C so as to produce the solid super acidic SO4<2-> / TiO2 catalyst. The method has the advantages that the method is economical in reaction, easy to separate the catalyst from products, little in corrosiveness on equipment, clean and free from pollution.

The invention discloses a method for preparing isoxazole compounds, using β-keto acid ester, α-diazoic acid ester and tert-butyl nitrite as reaction substrates, copper compounds as catalysts, Lewis acid as additives, three Ethylenediamine (DABCO) is a base, and the fully substituted oxazole product is prepared by a three-component reaction; the method used in the present invention has the following characteristics: the reactivity of the catalyst is high, the reaction conditions are mild, and the substrate has a wide range of applications. The post-treatment is convenient, the yield of the target product is high, the preparation process is simple, and the sources of raw materials used are extensive.

The invention discloses 1,2,4-triazole and a preparation method thereof. The 1,2,4-triazole is prepared by taking aryl diazonium fluoborate, a diazo ester derivative and organic nitrile as reaction substrates, taking transition metal as a catalyst and taking inorganic alkali as an additive through cyclization reaction. The method has the following characteristics: the reaction is more economic, the substrate universality is higher, late functionalization is realized easily, the reaction condition is mile, the reaction can be carried out in air, the use amount of the catalyst is small, aftertreatment is simple and convenient, and purification and industrialized application of products are facilitated. Meanwhile, the raw materials such as the reactants and the catalyst are cheap and easily available, the reaction composition is reasonable, ligand is not needed, the reaction steps are few, high yield can be obtained only by one-step reaction, the requirement and the direction of the contemporary green chemistry and medicine chemistry are met, and the preparation method is suitable for screening high-activity 1,2,4-triazole medicines.