24 results about "Cyanothymidine" patented technology

A multistep continuous flow synthesis method for the manufacture of isonicotinyl-hydrazide (Isoniazid) comprising reacting 4-cyano pyridine with NaOH at a specified molar ratio and temperature range to produce the intermediate isonicotinamide, which intermediate is reacted with hydrazine hydrate, without isolation thereof, at a specified molar ratio and temperature range to produce isonicotinyl-hydrazide (Isoniazid) in a yield greater than about 90%.

The invention discloses a synthesis process of a pyridine carbazole compound. Under the protection of nitrogen, a cyano carbazole compound is subjected to a redox reaction under the combined action of blue light, alkali, 4-cyanopyridine, TPP and a sacrificial agent DIPEA to form a pyridine carbazole compound; wherein the cyano carbazole compound is a derivative with a substituent R1 on a carbazole aromatic ring of 4CzIPN, and the substituent R1 is H, a methoxy group, a tertiary butyl group or a phenyl group; the alkali is inorganic alkali; according to the process, heteroarylation modification of the cyano carbazole photocatalyst is realized for the first time, the reaction yield is high, and the process has the characteristics of low cost, environment friendliness and safety in operation.

The invention discloses a 4-trifluoromethyl-3-cyanopyridine compound and an application of the 4-trifluoromethyl-3-cyanopyridine compound. The compound has a structure as shown in formula I, and the definition of each substituent group is as shown in the specification. The compound provided by the invention has excellent tumor cell proliferation inhibition activity and can be used for preparing antitumor drugs.

The invention discloses a purification method of 2-cyanopyridine, and belongs to the technical field of chemical engineering. The purification method of the 2-cyanopyridine comprises the following steps: in the process of preparing a 2-cyanopyridine crude product by taking 2-picoline as a raw material through ammonia oxygen catalysis, performing adsorption and impurity removal on the obtained 2-cyanopyridine crude product through an adsorption column filled with a metal adsorbent to obtain the pure 2-cyanopyridine, the metal adsorbent is formed by compounding two or more metals of Li, Cs, Be and Rb with graphene. According to the method, the 2-cyanopyridine with the purity of 99.8% can be purified to 99.99%, the high-quality 2-cyanopyridine is obtained, meanwhile, the reflux ratio does not need to be increased, the rectification energy consumption is reduced, and the cost is reduced; and moreover, the obtained high-quality 2-cyanopyridine is prolonged in preservation time, does not change color, and improves the market share.

The invention discloses a beta-pyridine alkyl phosphine sulfur compound as well as a preparation method and anti-tumor application thereof, and belongs to the technical field of organic synthesis and application. The structural formula of the beta-pyridine alkyl phosphine sulfur compound is shown in the specification. Wherein R1 is aryl or heteroaryl; r2 is methyl or hydrogen; r3 is methyl, chlorine or fluorine; and R4 is a phenyl group, a 3.5-dimethyl phenyl group or a cyclohexyl group. An olefin compound, a 4-cyanopyridine compound, powdered sulfur and a disubstituted phosphine hydrogen compound are used as reaction raw materials, alkali and a photocatalyst are added, a blue LED lamp irradiation reaction is performed in an inert atmosphere, and a reaction solution is concentrated, separated and purified to obtain the beta-pyridine alkyl phosphine sulfur compound. The beta-pyridine alkyl phosphine sulfur compound has human liver cancer cells HepG2 and has obvious anti-tumor activity.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to an intermediate for preparing elvanib, application of the intermediate and a method for preparing elvanib by using the intermediate. The invention relates to an intermediate for preparing elvanib and application of an intermediate 4 compound for preparing elvanib in preparation of elvanib, wherein the structural formula of the intermediate 4 compound is shown in the specification. According to the method, (S)-4-amino-5-(tert-butoxy)-5-oxovaleric acid, 2-bromo-4-cyanopyridine and the like which are low in cost are used as raw materials, and the reaction conditions of all the steps are mild. The synthesis method provided by the invention has the advantages of simple process steps, strong controllability, no need of tedious reaction and subsequent treatment processes, high yield, low cost and high product purity, and is suitable for industrial production.

The application provides a supercritical extraction process of 2-cyanopyridine, and the specific process steps comprise ammonia oxidation of 2-methylpyridine, supercritical extraction, and separation and purification. The extraction process can effectively solve the problems of general separation efficiency, poor product quality, and low yield in the current mainstream 2-cyanopyridine preparation process. The extraction process of the application avoids the use of sulfuric acid, and the production process is more environmentally friendly. The hydrolysis of 2-cyanopyridine is inhibited, the product yield is improved, the yield of 2-cyanopyridine reaches 88%, only a small amount of solvent material is left in the supercritical extraction extract, and the product quality is higher. The supercritical extraction achieves the purpose of extraction by changing the pressure and temperature, and the process is simple and the extraction speed is fast.

This invention discloses a pretreatment method for 3-cyanopyridine wastewater, belonging to the field of wastewater pretreatment technology. This method uses a modified magnetic porous adsorbent as its core and achieves continuous pretreatment of 3-cyanopyridine wastewater through a magnetically controlled adsorption separation device. The adsorbent uses a carboxyl-block polyarylene ether nitrile as a stable porous adsorption framework, introducing nitrile-carboxyl dual-target adsorption sites into the molecular chain. Simultaneously, graphene composite magnetic particles are introduced into the carboxyl-block polyarylene ether nitrile, providing rapid magnetic response separation performance. Through the deep synergy of highly selective adsorption and magnetically controlled separation, effective removal and resource recovery of 3-cyanopyridine are achieved. It can maintain stable treatment performance during long-term continuous operation and is suitable for the industrial pretreatment of 3-cyanopyridine production wastewater.

The invention discloses a synthesis method of 2-cyanopyridine, which belongs to the technical field of organic synthesis and comprises the following steps: step 1, adding a multi-component composite catalyst into an efficient reactor for reaction to obtain a reaction solution; 2, carrying out novel extraction separation on the reaction liquid obtained in the step 1 to obtain an extract liquid; and 3, carrying out deep separation and purification on the extract obtained in the step 2 to obtain the high-purity 2-cyanopyridine. According to the synthetic method of the 2-cyanopyridine, the green and environment-friendly ionic liquid is used for replacing a traditional harmful extraction agent to control pollution from the source, the yield is stabilized to be 90% or above by optimizing the reaction, catalysis and extraction processes, the product purity exceeds 99% by means of novel extraction and deep purification, the process is simplified by innovating equipment and the process, the period is shortened, and the method is suitable for industrial production. And finally, collaborative improvement of environmental protection, high efficiency, high quality and low cost is realized.

The present invention relates to hexahydropyrrolo[3,4-b]pyrrole-5(1H)-carbonitriles with activity as inhibitors of the deubiquitylating enzyme USP30, having utility in a variety of therapeutic areas, including conditions involving mitochondrial dysfunction, cancer and fibrosis.

The invention provides a 3-cyanopyridine compound as well as a preparation method and application thereof. The 3-cyanopyridine compound disclosed by the invention can be used as a fluorescent probe to show stable aggregation-induced emission (AIE) performance in an aggregation state. The 3-cyanopyridine compound has the advantages of high response speed, high selectivity and high sensitivity in the aspect of fluorescence detection of trace iron ions and nitro aromatic explosives, and can realize fluorescence detection of trace iron ions and nitro aromatic explosives in an aggregation state. The 3-cyanopyridine compound also has certain antibacterial activity, and has application potential in preparation of antibacterial drugs. The invention provides the preparation method of the 3-cyanopyridine compound, and the benzopyran nitrile compound which is easy to prepare is used as a raw material, inorganic base is selected, and a series of 3-cyanopyridine compounds are obtained through a series of cascade reactions. The synthesis method has the advantages of no need of metal catalysis, simplicity, feasibility, wide substrate application range, high yield and the like.

The application discloses a 3-cyanopyridine catalytic synthesis process based on a mesoporous molecular sieve, and belongs to the technical field of catalytic synthesis. The process takes 3-methylpyridine, ammonia and oxygen as main raw materials, and continuously synthesizes by relying on a composite mesoporous molecular sieve catalyst. The catalyst constructs a zirconium-cerium co-doped mesoporous silica framework in situ, improves the structural rigidity of the pore channel, and reduces the surface hydrophilicity. Meanwhile, in combination with the reduction and dissolution promotion of hypophosphorous acid and the strong complexation of phosphoric acid, vanadium sources are deeply penetrated into the mesoporous interior, so that the loss and failure of the active catalyst in a high-temperature hydrothermal environment are effectively avoided. Through the precise modification of the catalyst structure and the deep synergy of the continuous reaction conditions, the process realizes extremely high target product selectivity and excellent long-period anti-deactivation performance, and is suitable for large-scale industrialized continuous production of 3-cyanopyridine.

This invention discloses a method for synthesizing 4-bromo-3-cyanopyridine, comprising the following steps: (1) under alkaline conditions, oxidizing the hydroxyl group by phosphorus oxychloride to prepare the intermediate product 2-chloro-3-cyano-4-methoxypyridine; (2) placing the product obtained in step (1) in ethanol, adding palladium on carbon, and slowly introducing hydrogen gas into it to prepare the intermediate product 3-cyano-4-methoxypyridine; (3) adding phosphorus oxychloride to the acetonitrile solution of the product obtained in step (2) to prepare the target product 4-bromo-3-cyanopyridine. The synthesis method adopted in this invention has advantages such as readily available raw materials, mild reaction conditions, recyclable catalyst, no heavy metal pollution, and simple product post-processing, making it suitable for industrial production.

The invention relates to the technical field of fluorescence sensing and biological imaging, and particularly discloses a viscosity fluorescent probe based on an ESI PT mechanism as well as a preparation method and application of the viscosity fluorescent probe based on the ESI PT mechanism, and the molecular structure general formula is as follows: a large conjugated system with a rigid plane is used as a fluorophore, a proton donor group (hydroxyl-OH) and a proton acceptor group (azacyclo), the structural characteristics are used for ensuring that molecules can generate efficient intramolecular proton transfer in an excited state, and in addition, the specific electron withdrawing group-cyanopyridine salt is introduced in the molecular design of the probe, so that the molecular weight of the probe is increased, and the molecular weight of the probe is increased. And the fluorescence characteristic is highly sensitive to the viscosity change of the microenvironment. The ESIPT mechanism viscosity fluorescent probe has the advantages of high sensitivity, good biocompatibility, simple and convenient preparation method and the like, and can be used for detecting the viscosity change in human hepatoma cells HepG2 and zebrafish.

There is provided a process for the preparation of enantiomerically enriched pyridine compounds of formula (I) wherein R1 and R2 are as defined in the specification.

The invention comprises compounds of formula (I) wherein the groups R1 to R4 have the meanings given in the claims and the description, their use as KHK inhibitors, pharmaceutical compositions comprising compounds of this type and their use as medicaments, especially as agents for the treatment and / or prophylaxis of NAFLD, NASH and type II diabetes. # imgabs0 #

Provided are molecular probes for hyperpolarized 15N magnetic resonance spectroscopic imaging (MRSI) and their use for detecting reactive species (e.g., hydrogen peroxide) and imaging of oxidative stress. In particular, 15N-boronobenzyl-4-cyanopyridinium (15N-BBCP) demonstrated highly favorable physicochemical and hyperpolarization properties, including long spin-lattice relaxation time (T1) and distinguishable 15N chemical shift signals, that make it an effective reaction-based sensing probe for non-invasive, real-time detection of H2O2.

The invention discloses a method for preparing 2-cyanopyridine through fixed bed sectional temperature control, and belongs to the field of chemical engineering. The invention discloses a method for preparing 2-cyanopyridine by sectional temperature control of a fixed bed, which is characterized in that the reaction is controlled in a catalytic bed at multiple sections of different temperatures, the bed temperature is controlled, and side reactions are reduced, so that the yield of the prepared 2-cyanopyridine is more than or equal to 90%, the conversion rate of 2-methylpyridine is more than 99.9%, and the reaction selectivity is more than 90%.

The application discloses a preparation method of 2-cyanopyridine compounds, which comprises the following steps: taking a compound of formula I and a cyanation reagent as raw materials, and performing a cyanation reaction in a mixed system of water and an organic solvent in the presence of a catalyst and a ligand to obtain a compound of formula II, i.e. a 2-cyanopyridine compound; in the application, the cyanation reagent is widely available, low in price, safe and stable, the preparation method is simple and easy to operate, and the catalyst consumption is low; in the application, through the combination of the catalyst, the ligand and the organic solvent, high conversion of reactants can be realized, and high-purity products can be obtained, so that the application is suitable for large-scale production and wide application.

The invention discloses a colorimetric probe for detecting cyanide and a preparation method and application thereof, and the structural formula of the colorimetric probe is as follows: 4-cyano-2-pyridine-2-acetonitrile-1, 8-naphthalimide.

The invention discloses a method for synthesizing topinostat, and belongs to the technical field of synthesis of triazole heterocyclic compounds. The method is characterized in that the method comprises the following steps: using 4-cyanopyridine as a raw material, oxidizing to generate 4-cyanopyridine nitrogen oxide, and then performing Pinner condensation reaction to generate 4-((2N-isonicotinylhydrazide)carboxamidino)pyridine nitrogen oxide; then directly performing cyanation reaction to obtain N"-((2-cyanopyridine-4-yl)carboxamidino)isonicotinylhydrazide, and after the reaction, directly heating the reaction to generate intermolecular cyclization to construct the structure of triazole, generate topinostat, and then perform refining to obtain a topinostat fine product. The method adopts a "cyanation-cyclization" one-pot method to directly synthesize topinostat, and then performs refining to obtain topinostat with high purity. The synthesis method has simple steps, is convenient to operate, and has high yield and purity of the product.

The application discloses a kind of 3-cyanopyridine wastewater pretreatment methods, belong to wastewater pretreatment technical field, the method with modified magnetic porous adsorbent as core, and through magnetic control adsorption separation device realizes the continuous pretreatment of 3-cyanopyridine wastewater, the adsorbent with carboxyl-containing block polyarylether nitrile as stable porous adsorption skeleton, introduce nitrile group-carboxyl double targeted adsorption sites in molecular chain, while introducing graphene composite magnetic particles in carboxyl-containing block polyarylether nitrile, provide fast magnetic response separation performance, through the depth of high selectivity adsorption and magnetic control separation synergy, realize the effective removal and resource recycling of 3-cyanopyridine, can maintain stable processing performance in long-period continuous operation, suitable for industrialized pretreatment of 3-cyanopyridine production wastewater.

The present invention discloses a preparation method of 2,2'-bipyridine, which comprises the following steps: in the presence of a solvent, using 2-cyanopyridine and acetylene as raw materials, and catalytically cyclizing to form 2,2'-bipyridine in a microchannel reactor; the cyclization reaction temperature is 180-270 °C, and the cyclization reaction pressure is 0.2-0.7 Mpa. This preparation method is safe, environmentally friendly, and low in cost. The reaction materials are easy to handle, continuous production can be carried out, and high-purity products are easily obtained.

The present invention encompasses compounds of formula (I), wherein the substituents R1 to R4 have the meanings given in the claims and herein, their use as inhibitors of KHK inhibitors, pharmaceutical compositions comprising compounds of this type, and their use as medicaments, in particular as agents for the treatment and / or prevention of NAFLD, NASH and type 2 diabetes. JPEG2025539698000087.jpg59150