54results about "Amide group formation/introduction" patented technology

The invention belongs to the technical field of coupling reagents, and particularly discloses application of N-sulfonyl imidazolium salt as a coupling reagent, and the N-sulfonyl imidazolium salt as the coupling reagent is applied to synthesis of amide, dipeptide, polypeptide, carboxylic ester, carboxylic thioester, phosphamide and phosphate. According to the application of the N-sulfonyl imidazolium salt as the coupling reagent, compared with the prior art, the dosage of the coupling reagent is greatly reduced, the generation of byproducts is reduced, and the conversion rate of reactants is improved.

The invention relates to the technical field of organic chemical synthesis, and discloses a method for preparing a chlorogenic acid derivative by condensing chlorogenic acid and a bifunctional amino acid derivative, which comprises the following step: in the presence of EDCI and HOBt, reacting chlorogenic acid with the bifunctional amino acid derivative in a DMF solvent to obtain the chlorogenic acid derivative. The method does not need to protect hydroxyl, the synthesis steps are simple, and the reaction is green, environment-friendly and pollution-free.

The invention discloses an in-situ acetylation-co-crystallization method and application of the in-situ acetylation-co-crystallization method in organic molecular structure determination, and the in-situ acetylation-co-crystallization method comprises the following steps: synthesizing a cyclic trinuclear silver (I) complex as a crystallization partner, and carrying out an in-situ acetylation reaction in an organic molecular sample, after the reaction is completed, adding a crystallization partner for co-crystallization; the application of the in-situ acetylation-co-crystallization method in the determination of the organic molecular structure comprises the following steps: preparing a co-crystal from an organic molecule to be detected through the in-situ acetylation-co-crystallization method, collecting crystallographic data of the co-crystal, and analyzing to obtain a crystal structure of an acetylation product of the organic molecule to be detected; and determining the chemical structure and the spatial configuration of the to-be-detected organic molecule according to the crystal structure of the to-be-detected organic molecule acetylation product. The method can be used for structure determination of a series of acetylated organic molecules such as alcohols, phenols, amines and the like.

The present application relates to the field of chemical synthesis, in particular to a synthesis method of N-oxobutane acetamide and derivatives thereof.The synthesis method comprises the following steps: reacting a phenone compound with a nitrile compound, an acid and a reaction solvent to obtain the N-oxobutane acetamide and derivatives thereof; the phenone compound is p-bromophenone, p-fluorophenone, p-chlorophenone, p-iodophenone, p-cyanophenone, 3,4-dimethylphenone or 2-naphthaldehyde; the nitrile compound is acetonitrile, 3-chloropropionitrile, dichloroacetonitrile or deuterated acetonitrile; the acid is CF3SO3H or BF3; and the reaction solvent is acetonitrile or dichloroethane.The present application directly constructs the N-oxobutane acetamide and derivatives thereof in one step with the nitrile compound as the only nitrogen source, and has the advantages of cheap and easily available raw materials, mild conditions, high yield and easy scale-up production.

The present invention relates to a method for preparing of an amide of the formula (I-1) or a diamide of the formula (I-2) where the variables areas defined in the claims and the description, by reacting an ester with an aromatic or heteroaromatic amine in the presence of an alkali metal-containing base and a Lewis acid; where the reaction is carried out under essentially anhydrous conditions.

The present invention belongs to the field of chemical and chemical engineering technology, specifically a method for the continuous cleavage of alcohols into amides using a manganese oxide compound as a catalyst and molecular oxygen or air as an oxidant. The reaction is carried out at 130-150°C for 12 hours in the presence or absence of a solvent to oxidize the alcohols into amides. The catalyst can be recycled and reused at least nine times while maintaining excellent activity and selectivity. The catalyst is simple to prepare, inexpensive, highly selective, and environmentally friendly.

The invention discloses an amino acid derivatization method based on ester exchange and application of the amino acid derivatization method in bacterial amino acid stable carbon isotope measurement. According to the method, an alcoholic solution of boron trifluoride serves as a catalyst, carboxyl of amino acid reacts with ester groups in carboxylic ester, the ester groups are transferred to the amino acid, amino-acid ester is generated, and esterification of the carboxyl is achieved; and then carrying out acylation reaction on the amino-acid ester, triethylamine and acetic anhydride to realize acylation of amino groups. According to the method, chemical reagents causing damage to instruments do not need to be used, and generation of water in the reaction process can be avoided, so that the water removal step is omitted, the drying time is shortened, and meanwhile, side reactions and generation of by-products can be reduced. The method disclosed by the invention has good suitability with a stable isotope analysis instrument, can be used for rapidly and accurately determining the stable carbon isotope of the bacterial amino acid in an environmental sample, and has a wide application prospect in the aspects of establishing a bacterial amino acid monomer stable carbon isotope fingerprint database and widening an environmental microorganism traceability technical means.

The invention provides N-acylamino acid and application thereof, and relates to a novel compound and application thereof, the novel compound N-farnesyl acetyl amino acid or geranyl amino acid and application thereof, and the compound has remarkable 5 alpha reductase inhibitory activity, can promote hair growth and has low side effects. The N-(farnesyl acetyl or geranyl) amino acid provided by the invention has significant 5 alpha reductase inhibitory activity, and can effectively reduce DHT level, thereby promoting hair growth. Compared with the existing hair growth drug minoxidil, the compound provided by the invention has higher hair growth efficiency and lower side effects, and is expected to become a candidate drug of a new generation of hair growth drugs. The preparation method is simple, efficient and suitable for industrial production.

The invention relates to an acyl transfer reagent and a preparation method of an amide compound, and belongs to the field of organic synthesis in organic chemistry. Polyfluoro-substituted aromatic hydrocarbon, acyl chloride and a sulfur transfer reagent are adopted as raw materials, polyfluoro aryl thioester is obtained through two continuous electrophilic substitution reactions, and then further application research proves that the compound is an efficient acyl transfer reagent and can be used for acylation reactions of various amines. The route and reaction conditions adopted in the method are green, environment-friendly, simple and mild, the raw materials are easy to obtain, the product selectivity is high, the variety is rich, and the method is expected to be further applied to industrial production.

The invention relates to the technical field of drug screening, in particular to a completely-functionalized probe, a precursor of the completely-functionalized probe, a preparation method of the completely-functionalized probe, a probe library containing the completely-functionalized probe and a use method of the probe library. The completely functionalized probe is shown as a formula I or a formula II, wherein the formula I and the formula II are shown in the specification; lg is a ligand group containing a primary amino group, R1 does not exist or is-CH2-C (O)-, and R2 and R3 are reaction groups capable of reacting with nucleophilic residues of target protein. The fully-functionalized probe provided by the invention is convenient for high-flux synthesis, and overcomes the technical problems that the current fully-functionalized probe is limited by synthesis and sample preparation flux, and large-scale covalent ligand screening based on the fully-functionalized probe is difficult to realize.

The present application discloses a method and system for synthesizing amide compounds from nitrile compounds. The method for synthesizing amide compounds from nitrile compounds of the present application comprises dispersing nitrile compounds, photocatalysts and organic base additives in a mixed solvent of water and organic solvents, and performing a photocatalytic reaction under light in an atmosphere of oxygen or oxygen-containing atmosphere to generate amide compounds. The method for synthesizing amide compounds from nitrile compounds of the present application only requires adding a small amount of photocatalyst and using cheap and readily available oxygen as a reactant to efficiently obtain amide compounds; the reaction conditions are simple and mild, green and environmentally friendly, and easy to operate. The method of the present application can be applied to various nitrile compounds including aromatic nitriles, alkyl nitriles, and heterocyclic nitriles, and has strong applicability; moreover, it can be applied to microchannel reactors to meet the needs of large-scale industrial production.

Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.

The present invention relates to a method for coupling aryl halides with N-nucleophilic reagent compounds, characterized in that the coupling is carried out in the presence of a binuclear copper (II) complex with a substituted salbed-type ligand of formula (I). Also described are novel binuclear copper (II) complexes with a substituted salbed-type ligand within the scope of Formula (I).

The invention discloses a synthesis method for converting a Z-alkenyl amide compound into an E-alkenyl amide compound, and belongs to the technical field of organic synthesis. The method comprises the following steps: mixing and dissolving a Z-alkenyl amide compound and iodine in an organic solvent at room temperature, stirring for 10-30 minutes, and carrying out post-treatment on the obtained reaction liquid to obtain the E-alkenyl amide compound. Compared with a traditional alkene amide configuration isomerization method promoted by alkali in a hot solvent, the method disclosed by the invention has the advantages of simple materials, mild reaction conditions, short reaction time, high yield, simplicity and convenience in operation, easiness in solvent recovery and the like, and meets the requirements of developing green and environment-friendly chemistry; the substrate selection range and the functional group compatibility have wider universality, and the method can also be used for synthesizing natural products. The method is used for optimizing the synthesis strategy of part of drug molecules, can improve the synthesis efficiency and reduce the cost, and has industrial synthesis value and prospect.

Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure:or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.

The invention discloses a method for synthesizing an alkenyl amide compound through copper catalysis. According to the method, copper-based transition metal which is low in price and easy to obtain is used as a catalyst, silane is used as a reducing agent, and the synthesis of a target product is realized at high yield through reductive acylation and subsequent isomerization reaction between a ketoxime derivative and an acylation reagent under mild reaction conditions. The method has the advantages of mild reaction conditions, good functional group compatibility, wide substrate application range and the like. Besides, the catalyst and the reducing agent adopted in the method are low in cost, the method has remarkable economic advantages in large-scale synthesis, and a novel efficient and green method with practical value is provided for synthesis of the alkenyl amide compound.

The present invention discloses a method for preparing acrylamide compounds, and belongs to the technical field of organic synthesis. The present invention uses α-trifluoromethylstyrene, aliphatic amine, and water as raw materials, and a defluorination coupling substitution reaction occurs under the action of a catalyst to generate an acrylamide compound. The acrylamide compound synthesized by the method of the present invention has an acryloyl functional group and can be used as a synthetic precursor for many drugs and functional materials. The method of the present invention has very wide substrate adaptability, the starting raw materials α-trifluoromethylstyrene and aliphatic amine for the reaction are cheap and easily available, the reaction feeding process is simple, the post-reaction processing steps are simple, and it is suitable for industrial large-scale synthesis. It can provide a new method and new goal for the synthesis of drugs and the development of new materials.

The invention provides an N-trideuterium methyl benzisoxazole salt as well as a preparation method and application thereof. The N-trideuterium methyl benzisoxazole salt provided by the invention is applied to preparation of deuterated drug molecules, the preparation method is simple to operate, the use of transition metals and expensive ligands is avoided, the reaction economy is good, no by-product is generated in the reaction process, the atom economy is good, the reaction conditions are mild, safety and high efficiency are realized, and the N-trideuterium methyl benzisoxazole salt has good substrate applicability and is suitable for industrial production. And the method is widely applied to later-stage modification of drug molecules, and is suitable for large-scale production.

The application belongs to the technical field of organic synthesis, and particularly relates to a preparation method of a phenyl ketone amide compound. The preparation method of the phenyl ketone amide compound comprises the following steps: phenyl acylsilicon compound 1 and amide compound 2 are used as raw materials, a catalyst is added, and the phenyl ketone amide compound 3 is prepared by reacting in a first solvent. The reaction steps are short and efficient, the atomic utilization rate is higher, the yield of the obtained product is higher, the reaction condition is mild, the substrate range is wide, and the method is more suitable for industrial production.

The present invention relates to the field of synthetic organic chemistry, in particular to a process for preparing protected amines, such as blocked isocyanates and protected amino acids or amino acid esters. More in particular, the present invention relates to a process which is safer, practical and more environmentally friendly compared to those in the state of the art, and that avoids the use of phosgene, directly or indirectly, and free isocyanates. The present invention further relates to protected amines obtainable by the method, in particular to protected amino acids and amino acid esters. The present invention also relates to protected oligopeptides, and a method to prepare them starting from protected amino acids or amino acid esters.

The invention relates to a process for the coupling of an aryl halogenide with an N- nucleophile compound which is characterized in that the coupling takes place in the presence of a dinuclear copper(II) complex bearing substituted salben-type ligands having the formula (I). Also described are novel dinuclear copper(II) complex bearing substituted salben-type ligands within the scope of formula (I).

This invention discloses a method for synthesizing itaconic acid compounds. The method directly uses allyl ester compounds as raw materials, selects oxalic acid compounds or oxalate amine compounds as acylation reagents, uses triphenylphosphine as an additive, and employs metal-free 3,6,-di-tert-butyl-9-mesethyl-10-phenylacridine-10-tetrafluoroborate as a photo-redox catalyst. Under the catalysis of this organic photo-redox catalyst, corresponding acyl radicals and allyl radicals are generated, respectively. Through radical cross-coupling, itaconic acid compounds are finally obtained. This method has a wide range of applicable substrates, low preparation cost, and simple steps. It is convenient to operate, environmentally friendly, exhibits excellent stereoselectivity, and tolerates a broad spectrum of functional groups.

The invention relates to carrying out an enzymatically catalyzed condensation reaction in a hydrodynamic loop reactor with freely moving enzymes fixed to support particles and with a retention device for the catalyst particles. The loop reactor is fed via a mixer with a nozzle. The mixer with the nozzle mixes the liquid reactants immediately before they enter the reactor, without subjecting the catalyst to high shear forces. At the same time, the jet from the nozzle drives the free circulation of the catalyst particles in the loop reactor. The loop reactor reduces catalyst stress and denaturation and enables high conversion rates compared to other reactor designs. By using a hydrodynamic loop reactor with catalyst retention within the loop reactor, three-phase systems are avoided.

The invention relates to the field of chemical synthesis, in particular to a synthesis method of N-oxobutane acetamide and derivatives thereof. The synthesis method provided by the invention comprises the following steps: reacting an acetophenone compound with a nitrile compound, an acid and a reaction solvent to obtain N-oxobutane acetamide and the derivative thereof, the acetophenone compound is p-bromoacetophenone, p-fluoroacetophenone, p-chloroacetophenone, p-iodo acetophenone, p-cyano acetophenone, 3, 4-dimethyl acetophenone or 2-acetophenone; the nitrile compound is acetonitrile, 3-chloropropionitrile, dichloroacetonitrile or deuterated acetonitrile; the acid is CF3SO3H or BF3; the reaction solvent is acetonitrile or dichloroethane. The nitrile compound is used as the sole nitrogen source, N-oxobutane acetamide and the derivative thereof are directly constructed in one step, and the method has the advantages that raw materials are cheap and easy to obtain, conditions are mild, the yield is high, and large-scale production is easy.

The application discloses a carboxylic acid amidation method and an amide compound prepared by the method. The preparation method takes an amine compound and a carboxylic acid compound as raw materials, takes an organic solvent as a solvent, and performs light irradiation under the condition that a photocatalyst, an alkali and sulfur hexafluoride exist, so as to perform a reaction in the organic solvent to obtain the amide compound. The reaction condition of the application is mild, the reaction raw materials (including the amine compound, the carboxylic acid compound and the alkali) are cheap and easy to obtain, the application has the characteristics of cost saving, environmental friendliness and industrial popularization. The method effectively activates SF6, a greenhouse gas, and fully utilizes the decomposition products of SF6 to realize the amidation reaction of the carboxylic acid, so that SF6 is changed from waste to treasure. The required raw materials are simple and easy to obtain, the reaction condition is simple, green and energy-saving, and the application has high application value.