49results about How to "Synthetic method is convenient" patented technology

The invention discloses a method for synthesizing irbesartan and an intermediate thereof, and belongs to the technical field of preparation methods for medicines. The method comprises the following steps of: protecting 5-(4'-methylbiphenyl-2-yl)-2-(1-methyl-1-phenylethyl)tetrazole by using alpha-methyl styrene under the catalysis of organic acid through the novel convenient reaction process, brominating a benzyl group, condensing a solid phase and a liquid phase under phase transfer to obtain irbesartan protected by 1-methyl-1-phenylethyl, performing acid hydrolysis on the protection to obtain the irbesartan and 2-phenyl-2-propanol, and recovering the 2-phenyl-2-propanol to obtain the alpha-methyl styrene. The invention has the advantages that: the synthetic process is suitable for industrial production, economic value can be produced, the synthetic process is safe, the cost for raw materials is saved, the subsequent product can be easily treated, the reaction raw material is single, and the synthetic method is convenient.

The invention discloses a 2,6-dioxobicyclo[3.3.2]octane derivative and a synthesis method thereof. The synthesis method of the derivative is based on (E)-2-hydroxyl-1-naphthalene vinyl derivative The substrate is under the action of 1-chloromethyl-4-fluoro-1, 4-diazotized bicyclo[2.2.2]octane bis(tetrafluoroborate) salt and cuprous chloride, and the reaction obtains a novel 2,6-Dioxobicyclo[3.3.2]octane skeleton derivative compound. The method of the invention is simple to operate, and the reaction conditions are mild, and a novel 3D skeleton, two rings, three new chemical bonds (two C-O, one C-C) and four chiral centers are constructed in a one-pot reaction And a single stereo configuration was obtained, and a series of 2,6-dioxobicyclo[3.3.2]octane derivatives were constructed.

The invention discloses a bismuth sulfide / gadolinium oxide-entrapping ultrafine protein composite nanoparticle with a near-infrared photothermal effect and a multi-mode imaging function and a preparation method and application thereof. By formulation screening and process optimization, the bismuth sulfide / gadolinium oxide albumin ultrafine composite nanoparticle with the near-infrared photothermaleffect and the multi-mode imaging function is prepared in one step. The composite nanoparticle has good physicochemical stability, photostability, biocompatibility and tumor-targeting property, can remarkably enhance near-infrared fluorescence, photoacoustic, magnetic resonance, CT (computed tomography) and thermal signals at a tumor site, and realizes multi-mode-complemented tumor diagnosis, andmoreover, the composite nanoparticle can eliminate tumors under the excitation of near-infrared light; in particular, because the grain size of the nanoparticle is less than 5.5nm, the nanoparticle can be eliminated by the kidneys, and toxic and side effects are minor; a tumor can be diagnosed and treated at the same time, and the composite nanoparticle has a great potential in realizing accuratetumor diagnosis and treatment integration.

The invention discloses an asymmetric synthesis method of chiral compounds derived from trans-tetrahydrofuran / pyranotetrahydroquinoline. The method uses 5-o-hydroxyphenyl-4-ene-1-pentanol derivatives and o- The aminobenzaldehyde derivative is reacted under the action of a chiral phosphoric acid catalyst to obtain a chiral compound derived from trans-tetrahydrofuran / pyranotetrahydroquinoline. The present invention provides an efficient, simple and convenient method for the first synthesis of trans-tetrahydrofuran / pyranotetrahydroquinoline derived chiral compounds by adopting dearomatization, Prins cyclization and aza-Michael addition series reaction modes resolve resolution. The method of the invention is simple to operate, and the reaction conditions are mild, and two new heterocycles, three new chemical bonds (C-O, C-C, C-N) and three adjacent quaternary carbon chirals are constructed in the one-pot reaction. A series of chiral compounds derived from trans-tetrahydrofuran / pyranotetrahydroquinoline were constructed.

The invention discloses a nano-cuprous oxide / silk fibroin complex and a preparation method thereof, which is characterized in that the main raw materials for preparing the complex include: 1.0-2.0 parts of silk fibroin, copper sulfate pentahydrate 0.5-2 parts, sodium hydroxide 0.58-1.92, vitamin C 0.7-2.8 parts. The preparation steps include: dissolving silk fibroin in deionized water to prepare a silk fibroin solution; preparing copper sulfate pentahydrate into a copper sulfate solution, adding it to the silk fibroin solution and stirring evenly, and then adding sodium hydroxide solution to adjust the pH value 10-12; vitamin C is formulated into a solution and added to the solution obtained in the above step (2), reacted at room temperature for 30-60 hours, dialyzed for 2-4 days, and freeze-dried to obtain nano-cuprous oxide / silk fibroin porous sponge. It can effectively hinder the agglomeration of nano-cuprous oxide particles, increase the stability of nano-cuprous oxide, prevent its oxidation, and prepare materials with various shapes.

The invention discloses a synthesis method of 4-allyl-3,5-disubstituted isoxazole, belonging to the technical field of organic synthesis. The synthesis method is as follows: in the reactor, add acetylene ketoxime ether substrate, 3-bromopropene, palladium catalyst, additive and solvent, stir and react at 70-80°C, and the reaction product is separated and purified to obtain 4-allyl -3,5-disubstituted isoxazoles. In the method of the present invention, a series of acetylenic ketone oxime ethers are obtained by reacting the product obtained through Sonogashira coupling of simple and easy-to-obtain acyl chlorides and alkynes with methoxyamine hydrochloride, the reaction conditions are mild, and there is no pollution to the environment. Potentially functional 4-allyl-3,5-disubstituted isoxazole compounds, the method is innovative and atom-economical, mild conditions, safe operation, and can be scaled up to 5 g scale without affecting the yield Therefore, it has potential practical value.

The invention discloses a polypyrrole / nickel hydroxide / foamed nickel integrated electrode and preparation method thereof. The polypyrrole / nickel hydroxide / foamed nickel integrated electrode is formed by loading foamed nickel with polypyrrole and nickel hydroxide, the total load amount of the polypyrrole and the nickel hydroxide on the foamed nickel is 0.9% to 1.4%, and the mass ratio of the polypyrrole to the nickel hydroxide is 1:3 to 2:1. An electrochemical test is performed on the integrated electrode, the electrode has excellent electrochemical performance, as the amount of polypyrrole increases, the specific capacitance of a material increases first and then decreases, and when the molar ratio of nickel nitrate to hexamine is 1:1 and the pyrrole monomer concentration is 0.05mol L<-1>, the specific capacitance of the electrode under the electric current density of 2A g<-1> reaches up to 2174F g<-1>, and the highest specific capacitance retention rate is achieved.