206 results about "Pyrroline" patented technology

The invention relates to sulfonyl-containing 3,4-diaryl-3-pyrrolin-2-ones compounds having formula (I) wherein R1 is selected from the group consisting of 4-methylsulfonyl, 4-aminosulfonyl, hydrogen, 2-, 3-, or 4-halogen, C1-C6-alkyl, cyclopentyl, cyclohexyl, C1-C4-alkoxy, hydroxy, cyano, nitro, amino or trifluoromethyl; R2 is selected from the group consisting of 4-methylsulfonyl, 4-aminosulfonyl, hydrogen, 2-, 3-, or 4-halogen, C1-C6-alkyl, cyclopentyl, cyclohexyl, C1-C4-alkoxy, hydroxy, cyano, nitro, amino or trifluoromethyl; and R3 is selected from the group consisting of hydrogen, methyl, ethyl, n-propyl, i-propyl, c-propyl, n-butyl, isobutyl; provided that when R1 is a methylsulfonyl or aminosulfonyl group, R2 is any group as defined above except a methylsulfonyl or aminosulfonyl group; and when R2 is a methylsulfonyl or aminosulfonyl group, R1 is any group as defined above except a methylsulfonyl or aminosulfonyl group, also to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the medical use of such compounds in the treatment of diseases relating to the inhibition of cyclooxygenase-2 (COX-2).

The invention relates to an organic second-order non-linear optical chromophore with a D-Pi-A structure and decorated by a tree-like group, and a synthesizing method and applications thereof. The chromophore of the invention introduces a thiophene ring conjugated Pi electronbridge having stronger electrical transmission capacity and containing branched chains and a tricyano pyrroline receptor having strong electron-withdrawing property; the receptor end is introduced into the tree-like decorative group, the one-order hyperpolarizability of chromophore molecules is greatly improved; the solubility and the film forming ability of the chromophore in polymer is improved, the interaction force among the molecules is reduced. The second-order non-linear optical chromophore with the following structure is doped with polymers, such as amorphous polycarbonate or polymethylmethacrylate and the like according to the mass ratio of 1:10; the electro-optical coefficient of the obtained polarized polymeric materials achieves 217pm/V; in addition, the donor and receptor of the chromophore can be introduced into a crosslinkable group, thus improving oriented stability of the chromophore in polymer, and satisfying the requirements of devices.

The present invention provides a process for preparing of 2-acetyl-1-pyrroline, the principle aroma component of basmati and other varieties of scented rice, and also of processed cereal and grain products, said flavor chemical is of great value, in the art of application of flavor to foodstuffs like rice and bakery products.

The invention discloses a triphosgene method for synthesizing benzene sulphanilamide, the intermediate of glimepiride, a drug for Type ii Diabetes Mellitus. Triphosgene is slowly dropped into a solution which contains phenethylamine and 3-ethyl-4-methyl pyrroline ketone, at a controlled temperature, so that N-[2-(3-ethyl-4-methyl-2-oxidation-3-pyrroline-1-formylamino)ethyl]-benzene (3) is obtained; the product reacts with chlorosulfonic acid to generate sulfonated product; the sulfonated product reacts with ammonia water to generate crude product benzenesulfonamide; the crude product is refined through solvent treatment to generate fine product; the reaction formula is show in the specification. The triphosgene method is simple in technology, simple in operation and high in yield; compared with the conventional method of phosgene, the solid phosgene (triphosgene) method is safer and is convenient to operate.

The invention discloses a preparation method of Glimepiride raw material, which comprises the following steps in sequence: in the presence of K2CO3, a condensation reaction is carried out between a compound A: 4-[2-(3-ethyl-4-methyl-2-keto-3-pyrroline-1-formamido)-ethyl]-benzene sulfonamide and a compound B: trans-4-methyl-cyclohexyl isocyanate of the same molar weight in an organic solvent. The mass ratio of the compound A and K2CO3 is 1:0.8-0.9; the mixture synthetic fluid of a crude Glimepiride product and K2CO3 is filtered in a suction way, and then an extract is added into pure water and dissolved to form a solution. The solution is filtered for removing impurities to obtain the aqueous solution of Glimepiride; a hydrochloric acid solution is added into the aqueous solution of the Glimepiride for acidification and then a crude product is separated; acetone is added into the crude Glimepiride product and then refined, filtered in a suction manner, dried in a vacuum environment to obtain a pure Glimepiride product. The method has the advantages of simplifying the synthetic route, selecting mature intermediates as raw materials, adding K2CO3 for promoting the condensation reaction, avoiding the use of chloroform, reducing the residual organic solvent, and being applicable to industrialized production.

Immunotherapy comprises administration of an alkaloid at a dose sufficient to induce IL-2 production in dendritic cells in a patient. The alkaloid induces the production of IL-2 in dendritic cells. The alkaloids need not be naturally occurring, and may be synthetic analogues or derivatives of naturally occurring counterparts. Such analogues or derivatives are preferably pharmaceutically acceptable analogues, salts, isomers or derivatives as herein defined. However, preferred alkaloids are phytochemicals. Such phytochemicals may be isolated from natural sources or synthesised in vitro. Particularly preferred are alkaloids is selected from piperidine alkaloids; pyrrolin alkaloids; pyrrolidine alkaloids; pyrolizidine alkaloids: indolizidine alkaloids and nortropane alkaloids.

The invention relates to a 5-fluoro polysubstituted pyrroline derivative of the structure shown as the formula (III). According to a preparation method of the 5-fluoro polysubstituted pyrroline derivative, under the action of alkali, a trifluoromethyl-containing alkene compound and an amide diethyl malonate compound are subjected to a cyclization reaction, extraction, concentration and column chromatography to obtain the 5-fluoro polysubstituted pyrroline derivative; the reaction process is shown as the reaction formula (1). Through the preparation method, reaction conditions are mild, operation is simple, and a structural framework of a 5-fluoro polysubstituted pyrroline compound is obtained. Please see the description for the reaction formula (1).

The invention relates to the technical field of food processing, and discloses a pandanus amaryllifolius product and a preparation method thereof. The preparation method disclosed by the invention comprises the following steps: pre-freezing pandanus amaryllifolius leaves; pre-freezing the pandanus amaryllifolius leaves, then performing freeze-drying under a vacuum condition, performing heating to40-50 DEG C at a constant speed, and performing heat preservation; reducing the temperature to 35-45 DEG C for the first time at a constant speed, and performing heat preservation; and reducing the temperature to 30-40 DEG C for the second time at a constant speed, and performing heat preservation to obtain the pandanus amaryllifolius product. According to the process provided by the invention, the technical methods of ultralow temperature freezing, uniform temperature rising and drying and the like are adopted to realize color preservation and fragrance enhancement of pandanus amaryllifolius,and the prepared pandanus amaryllifolius product has the characteristics of high content of substances such as 2-acetyl-1-pyrroline, leaf green alcohol, squalene and the like, can effectively protectnatural green color of the pandanus amaryllifolius, and provides technical support for large-scale production of pandanus amaryllifolius.

The invention discloses a synthetic method for pyrroline-3-formic ether compounds, and belongs to the technical field of organic synthesis. The technical key point of the synthetic method is disclosed in the following diagram. Compared with the prior art, the synthetic method has the following advantages: (1) one-pot cascade reaction is adopted so as to avoid a complex intermediate separation and purification process, reduce waste emission and lower environment burdens; (2) raw materials can be easily obtained; (3) reaction is carried out below 100 DEG C, conditions are moderate, and operation is simple; (4) the applicable range of a substrate is wide; (5) the economy of reacting atoms is high.

The present invention discloses a method of synthesizing multi-hydroxy pyrrolidine alkaloid. The present invention comprises the following steps: 1) the multi-hydroxy ring-shaped nitrone of the structure in formula II reacts to prepare Cbz-protected amide of the structure in formula III; 2) the amide of the structure in formula III is changed into an alpha, beta-unsaturated ketone of the structure IV; 3) the alpha, beta-unsaturated ketone of the structure IV and ketone do the dual-hydroxylation reaction with the influence of osmium tetroxide and NMO system to get a structure in formula V; 4) the formula V is catalyzed and hydrogenated to get the multi-hydroxy pyrrolidine alkaloid of the structure in formula I. The present invention startes from the low-cost and easily accessible raw materials; the sugar derived multi-hydroxy chiral nitrone is used as a key chiral intermediate; a set of simple, effective and practical methods of highly three-dimensional selectivity and high production rate to synthesize the multi-hydroxy pyrrolidine alkaloid of hyacinthacine C₁ category is formed through the pro-nuclear addition, Wittig reaction, double-hydroxylation and reductive amination and other reactions.

Provided are novel water containing active hydrogen wherein the content of active hydrogen is high and a process wherein such active hydrogen-containing water is produced simply at high efficiency from an inexpensive material without needing complex apparatus or special treating agents. The water containing active hydrogen of the present invention with respect to which, in an electron spin resonance spectrum pattern obtained by measuring under such a condition that immediately after generation treatment of hydrogen radicals, 25% by mass of 5,5-dimethyl-1-pyrroline-N-oxide is added to thereby stabilize hydrogen radicals, the intensities of peaks ascribed to hydrogen radicals occurring in the vicinity of 331.8 mT magnetic field strength and in the vicinity of 335.5 mT magnetic field strength are 0.03 or greater and 0.04 or greater, respectively, taking the intensity of peak ascribed to manganese as the standard sample is produced by bringing the starting water into contact with activated carbon carrying a water-insoluble ferric oxide hydrate after a magnetization treatment.

A granular imidacloprid with high effect and solubility is prepared from imidacloprid, dichlorvos, carrier (sand) and strong adsorbent through adsorbing imidacloprid and dichlorvos by strong adsorbent, coating by PVC or paraffin wax, and baking.

The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): Formula (I), R<2> is selected from the group consisting of -C1-8alkyl-Z, -C2-8alkenyl-Z and -C2-8alkynyl-Z; wherein the -C1-8alkyl-Z, -C2-8alkenyl-Z and -C2-8alkynyl-Z and Z is a 5 to 6 member aromatic monocyclic heteroaryl ring having from 2 to 4 heteroatoms. These compounds are useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.

The invention provides an oxiracetam preparation technology, which is characterized in that 4-methoxy-pyrroline-2-ketone-1-yl-acetic acid is taken as an initial raw material, and four steps of deprotection, reduction, esterification and aminolysis are carried out to obtain the target product-oxiracetam. the steps of deprotection, reduction, esterification and aminolysis are realized by using an one-pot method, the overall yield reaches as high as 52.5%, and the yield is more than 30% compared with the documented yield. The application of the one-pot method can effectively simplify the operation step and shorten the production period, the generation of side effect can be avoided, and the three wastes discharge capacity can be greatly reduced, the environmental pollution is reduced, the route can greatly reduce the cost of the bulk drug, and the preparation technology is a production route having an industrialized prospect.

The invention provides a method for preparing (S)-2-(3-pyridine)-pyrrolidine. The chiral 2-pyridine pyrrolidine compound is prepared by utilizing imine reductase (IRED) or engineering bacteria for expressing the imine reductase (IRED). A glucose dehydrogenase/glucose system is utilized to realize regeneration of coenzyme. More specifically, the invention provides a method for reducing a 2-pyridine-1-pyrroline compound into (S)-2-(3-pyridine)-pyrrolidine by utilizing the imine reductase derived from Myxococcus fulvus and a genetically engineered bacterium thereof, the imine reductase derived from Myxococcus fulvus is relatively high in activity, relatively high in reaction substrate concentration, relatively high in reaction yield and relatively high in optical purity of a product, In the reaction process, operation is easy, energy consumption is low, the green chemical requirement is met, and the method can be applied to biotransformation preparation of the (S)-2-(3-pyridine)-pyrrolidine compound in industrial production.

The invention discloses a synthesis method of a penta-substituted 2-amino-2-pyrroline derivative. In an organic medium with higher polarity, the aryl propionate of ortho-amino halide and malononitrile are enabled to generate a nucleophilic substitution reaction and a nucleophilic ring closing reaction once under the action of an alkali; the penta-substituted 2-amino-2-pyrroline derivative is obtained in one step. According to the synthesis method, a common alkali which is low in cost is adopted as an accelerant; the cost is effectively decreased; further, no matter that the aryl propionate of the ortho-amino halide is the aryl propionate of alpha-amino-beta halide or alpha-halide-beta-amino, the amino in a synthesized product is always located at the 2-site of the ring of pyrroline; carbon-carbon double bonds in the pyrroline are both located at a 2-site and 3-site; the 2-amino-2-pyrroline derivative has high regioselectivity. The selection of a substituent group in the 2-amino-2-pyrroline derivative synthesized by the synthesis method has higher flexibility; the 2- site amino and the 3-site cyano can generate a 4+1 or 4+2 cyclization reaction; the 2-amino-2-pyrroline derivative can be used for the fields of the synthesis of fused heterocyclic compounds, natural antibiotics and anti-cancer drugs and the research of the structural modification of natural products.

There is provided an organic nonlinear optical material including a polymer binder and a compound represented by the following Formula (I):

Provided is a dye for photoelectric conversion containing at least one or more kind of a compound represented by the following General Formula (1) (in Formula (1), R¹ and R² represent any one of —CN, —SO₂R, —COOR, and —CONR₂ (R represents a hydrogen atom, a substituted or unsubstituted alkyl group, a cycloalkyl group, or an aryl group); R³ represents a direct bond or a substituted or unsubstituted alkylene group; X represents an acidic group; and D represents an organic group having an electron donating substituent or a substituted or unsubstituted heterocyclic group).

The invention relates to a method for compounding a pyrroline derivative in one step by cyclizing and coupling suzuki and belongs to the field of chemical compounding of allene (1,2-propadiene) by cyclizing. The method is characterized in that (1) transition metal elements are adopted for catalyzing; (2) allene is used as a raw material for compounding; (3) the reaction is performed when the reaction temperature is low temperature or normal temperature; (4) the reaction is completed in one step; (5) the catalyst is fully recycled; (6) water is strictly removed from a reaction solvent and the trace level is achieved; (7) 2,3-pyrroline five-element ring is the main structure of the generated product; (8) the physical and chemical properties of the generated product are not changed under normal temperature and high temperature environments; (9) the yield of the generated product is more than or equal to 98 wt%; (10) the generated side products are easily removed according to a conventional method.