57 results about "Dimethylpiperidone" patented technology

The invention mainly relates to a synthesis method of alvimopan. A preparation method of the related alvimopan comprises the following steps of: condensing phenylpropionic acid and substituted oxazolidone; undergoing reaction with chloromethyl benzyl ether under the action of a catalyst to obtain a single configuration; hydrolyzing, and recycling oxazolidone to obtain carboxylic acid; condensing with glycinate; performing deprotection and undergoing reaction with a leaving group donor; butting with (+)-(3R,4R)-4-(3-hydroxy phenyl)-3,4-dimethyl piperidine to obtain alvimopan ester; and hydrolyzing to obtain the alvimopan. The invention also relates to a novel intermediate of the alvimopan and preparation methods of the alvimopan and the novel intermediate of the alvimopan. The technical scheme of the invention has the advantages of simple process, low cost and high product purity, and is suitable for industrial production.

The invention relates to a novel preparation method of a tofacitinib intermediate and in particular to a preparation method of the tofacitinib intermediate (3R,4R)-1-benzyl-N-4-dimethyl piperidine-3-amine dihydrochloride. The preparation method comprises the following steps of: by taking 1-benzyl-4-methyl-1,2,3,6-tetrahydropyridine as an initial raw material, oxidizing olefin to form a ketone II by means of a one-step process; forming imine III with amine; applying asymmetric reduction imine to form amine; removing a trans isomer by recrystallization to obtain a cis-form structure IV; and finally, applying chiral resolution to obtain a final product (3R,4R)-1-benzyl-N-4-dimethyl piperidine-3-amine dihydrochloride I. The preparation method is creative in process, the process steps are shortened, and the synthetic yield of an asymmetric compound is greatly increased, thereby laying a solid foundation for industrial production.

The present invention relates to a novel preparation method of a tofacitinib intermediate bis-(3R,4R)-1-benzyl-N,4-dimethyl piperidin-3-amine L-di-p-toluyl tartrate. According to the preparation method, 3-amino-4-methyl piperidine is adopted as a starting raw material, is subjected to a N-methoxycarbonylation reaction under the sodium hydride effect, and is subjected to a catalytic hydrogenation reaction, a nucleophilic substitution reaction, an amide reduction reaction under the red aluminum effect, and L-di-p-toluyl tartaric acid (L-DTTA) chiral splitting so as to finally prepare the target compound bis-(3R,4R)-1-benzyl-N,4-dimethyl piperidin-3-amine L-di-p-toluyl tartrate. The process of the present invention has characteristics of further existing process improving, simple operation, easy post-treatment, high yield, and low cost.

This invention provides a harmful organism control composition having an excellent harmful organism control effect and comprising as an effective ingredient the following 4-(2-butynyloxy)-5-fluoro-6-(3,5-dimethylpiperidino)-pyrimidine (X):and a hydrazide compound represented by formula (I):wherein A1 and A2 represent, for example, an oxygen atom; R1, R2, and R3 represent, for example, a hydrogen atom, a C1-6 alkyl group optionally substituted by a halogen atom; and Q represents, for example, a methoxycarbonyl group.

The invention relates to the field of synthesis of catalytic materials and discloses a synthesis method and an application of an AEN-structured Si-P-Al molecular sieve. The synthesis method comprisesa mode one: a mixed solution containing a P source, an Al source, a Si source, a structure-directing agent and water is subjected to hydrothermal crystallization with a hydrothermal method and then issubjected to solid-liquid separation and dried; a mode two: a mixed solution A containing the P source, the Al source and water is aged and dried with a P-Al dry glue liquid phase conversion method,and dry P-Al glue is prepared; a raw material mixture B containing the dry P-Al glue, the Si source, the structure-directing agent and water is subjected to hydrothermal crystallization, solid-liquidseparation and drying, wherein the structure-directing agent is 1-methyl-4-piperidinone and / or 1,3-dimethyl-4-piperidone. According to the synthesis system, the AEN-structured Si-P-Al molecular sieveis easy to synthesize. The AEN-structured Si-P-Al molecular sieve synthesized with the method can be applied to storage of small molecule gases such as hydrogen, methane and the like, can also be usedfor gas absorption separation and has good application prospect.

The invention discloses a (+)-(3R,4R)-[[2S-[[4-(3-hydroxyphenyl-3,4- dimethyl-1-nipecotic)-methyl]-1-oxo-3-phenylpropyl]amido]benzyl cetate compound and its process for preparing and a new technology for preparation of Mope by the said compound. The new technique of this invention changes the 'one chain' synthesis of the original patent method to the separate 'two chains' preparation, by which the total compound steps are dramatically shortened, the compound cost is reduced to about one-half of the original patent method, and the method is more competitive on the market in price. Furthermore,the reaction condition is moderate, the operating procedure is simple, each reaction step is no need of given condition such as low temperature and absolute water-free, so it is more suitable for industrial production.

Disclosed is a single step process for separating Cis-3,5-dimethylpiperidine from a mixture of its geometrical isomers. The method comprises hydrogenation of 3,5-lutidine in the presence of water and 5% ruthenium on alumina as the catalyst at a predetermined range of temperature and pressure and does not involve the use of any organic solvent.

Novel 3,4-disubstituted-4-(3-carbamoylphenyl)-piperidinylpropanoic acid compounds and their salts, including pharmaceutically acceptable salts, pharmaceutical compositions and methods of their use are disclosed. The novel compounds are useful, inter alia, as antagonists of opioid receptors.

The present invention relates to crystalline forms of (9E,10E)-2,7-bis((3,5-dimethylpiperidin-1-yl)sulfonyl)anthracene-9,10-dione dioxime, pharmaceutical compositions comprising the crystalline form, processes for preparing the crystalline form and methods of use therefore.

The invention discloses a method for synthesizing a chiral tofacitinib citrate intermediate by an enzymic method. The method comprises the following steps: by taking 4-methyl-1-(phenyl methyl)-3-piperidone (TOF15) as a raw material, performing biological catalysis to obtain a chiral intermediate TOF 20-A, and then performing methylation reaction to obtain an intermediate TOF 25-A, namely free (3R, 4R)-1-benzyl-N, 4-dimethyl piperidine-3-amine, wherein the intermediate TOF 25-A can be further made into hydrochloride, so that (3R, 4R)-1-benzyl-N, 4-dimethyl piperidine-3-amine dihydrochloride (TOF30) can be obtained. The method is a synthesis technology which is low in cost, high in yield and environment-friendly, is suitable for large-scale industrial production, and has huge market application value.

The invention relates to a making method and an application of a polythiophene derivative electrochemiluminescence sensor. In the invention, a polythiophene derivative poly(3-1,1'-dimethyl-4-piperidylmethylene)-2,5- chlorothiophene) is used as a luminescence material, has good water solubility and good optical performances, and is in favor of constructing sensitive and stable electrochemiluminescence sensors. Bromate ions are used as a coreactant of an electrochemiluminescence reaction of poly(3-1,1'-dimethyl-4-piperidylmethylene)-2,5- chlorothiophene) due to the oxidation of the bromate ions, and the electrochemiluminescence intensity varies with the concentration of the bromate ions in order to detect the bromate ions. The potassium bromate electrochemiluminescence sensor made in the invention has the characteristics of simplicity, rapidness and sensitiveness, and is suitable for the rapid detection of potassium bromate in drinking water and river water.

The invention belongs to the technical field of cotton production, and particularly relates to a cotton topping agent and preparation and application methods thereof. The cotton topping agent comprises the following components in percentage by mass: 35-45% of a first component and 55-65% of a second component, wherein the first component is 2-chloroethyl trimethyl ammonium chloride and / or N, N-dimethyl piperidine ammonium chloride; the second component is carbamoyl ethyl phosphate ammonium salt and / or N-(2-chloro-fluorobenzyl)-N-ethyl-alpha, alpha, alpha-trifluoro-2, 6-dinitro-p-toluidine, andthe result shows that the chemical topping agent is suitable for an environment with high temperature, much rainwater and high humidity, and can obviously reduce the plant height of newly born main stems and fruit branches of cotton and increase the boll number of a single plant; the chlorophyll content of leaves is increased, and the photosynthetic intensity is remarkably enhanced; the falling rate of cotton buds and bolls is reduced, and the seed cotton yield is increased; and labor investment can be saved by more than 0.5 per mu.

The invention relates to a preparation method of high-purity cis-3,5-dimethylpiperidine, belonging to the field of organic synthesis. Using 3,5-lutidine as a raw material, 3,5-dimethylpyridine is obtained through catalytic hydrogenation reaction. The crude methylpiperidine is purified by precipitation to obtain high-purity cis-3,5-dimethylpiperidine, and its cis gas chromatographic purity is more than 99.5%. In the present invention, by introducing neutral alumina and alkali, the combination mode of pyridine molecules and catalyst molecules in the hydrogenation process is changed, which is beneficial to the generation of cis-isomers, and can obtain crude products directly used in pharmaceutical production; 99.5% of the cis isomer, there is no such high-purity report in the synthesis and separation of 3,5-dimethylpiperidine cis, in the synthesis and purification of piperidine derivatives and industrial production applications, it has greater Reference significance and high commercial value.