43 results about "Glutaconate" patented technology

The invention relates to a new synthesis technology of anti-cancer drug Raltitrexed. The technology comprises the following steps: 1) using L-glutamic acid as raw material to perform esterification with alcohol under the action of halogenating agent and obtain L-glutamic acid diester hydrochloride; 2) using 2-amino-5-methyl-benzoic acid as raw material to prepare 6-bromomethyl-3,4-dihydro-2-methyl-4-oxo-6-quinazoline through cyclization, amination and bromination; 3) using 2-thienyl-propanedioic acid as raw material to prepare N-[5-[N-(tert-butoxycarbonyl)-N-methylamino]-2-thenoyl]-L-glutamic acid diethyl ester through nitrification, esterification, reduction, amino protection, N-methylation and device-esterification; 4) using L-glutamic acid diester hydrochloride and N-[5-[N-(tert-butoxycarbonyl)-N-methylamino]-2-thenoyl]-L-glutamic acid diethyl ester to prepare N-[5-(N-methylamino)-2-thenoyl]-L-glutamic acid diester through dehydrant condensation and deamination protection; and 5) using N-[5-(N-methylamino)-2-thenoyl]-L-glutamic acid diester and 6-bromomethyl-3,4-dihydro-2-methyl-4-oxo-6-quinazoline to perform condensation under the catalysis of alkali, recycling preparative chromatography, purifying, and performing de-esterification to obtain Raltitrexed.

The present invention relates to a moisturizer comprising γ-polyglutamic acid (γ-PGA, H form), and / or one or more of its salts (i.e., γ-polyglutamate in Na+ form, γ-polyglutamate in K+ form, γ-polyglutamate in NH4+ form, γ-polyglutamate in Mg++ form, γ-polyglutamate in Ca++ form) and / or γ-polyglutamate hydrogel, wherein said moisturizer is used in cosmetic products or personal care products.

The invention relates to a preparation method and an application of a double-rate-type (ultraviolet / fluorescence) multifunctional (calorimetric / fluorescence / ultraviolet) high-sensitivity florescent probe for carboxylesterase detection. Firstly, 2,4-dihydroxybenzaldehyde, diethyl glutaconate and anhydrous piperidine react in ethyl alcohol to produce a product 1, the product 1 and acetic anhydride react in anhydrous pyridine to produce a product 2, the product 2 reacts with osmium tetroxide and sodium periodate in tetrahydrofuran to produce a product 3, and the product 3 reacts with anhydrous potassium carbonate in methyl alcohol to produce a product 4; then methylpyridine and methyl iodide react in absolute ether to produce a product 5; next, the product 4 and the product 5 are dissolved in absolute ethanol, piperidine is added for a reaction, and a product 6 is obtained; finally, the product 6 is dissolved in acetic anhydride, anhydrous sodium acetate is added, and the double-rate-type multifunctional florescent probe for carboxylesterase detection is obtained. The probe is applicable to qualitative and quantitative analysis of carboxylesterase in biological samples, is sensitive, accurate and quick in detection, and can be applied to related fields of analytical chemistry, life organic analytical chemistry, disease pre-diagnosis, clinical medical examination and the like.

The invention relates to a preparation method of high-purity palbociclib. The method comprises using acetoacetate for reflux dehydration in the function of an acid catalyst to prepare 2-acetyl-3-methyl-2-diethyl (methyl) glutaconate (III), condensing the compound (III) and trimethyl orthoformate for methanol removal to obtain 2-acetyl-3-methyl-4-methoxymethylene-2-diethyl (methyl) glutaconate (IV), cyclizing the compound (IV) and N-(5-(4-tertbutoxycarbonyl-1-hexahydropiperazinyl)-2-pyridyl) guanidine (V) with pyrimidine to obtain 2-acetyl-3-[[5-(4-tertbutoxycarbonylpiperazinyl-1-yl) pyridine-2-yl] amino]-3H-4-one-dihydropiperazinyl-2-ethyl (methyl) butenyl ester (VI), and finally cyclizing the compound (VI) and cyclopentylamine to remove Boc protecting groups, thereby obtaining palbociclib. The preparation method is cheap and available in raw materials, short in technical process, simple and convenient to operate, good in reaction selectivity, and high in product yield and purity and is green and eco-friendly.

The invention discloses a synthetic method of pyrroloquinoline quinone. The synthetic method comprises the following steps: carrying out alkali treatment on 2-methoxy-5-nitroaniline hydrochloride as a raw material, so as to obtain a compound 1; carrying out formylation on the compound 1 under a catalysis condition of an ionic liquid, so as to obtain a compound 2; adopting sodium borohydride to reduce the compound 2 to obtain a compound 3; carrying out diazotization on the compound 3, and then enabling action between the diazotized compound 3 and HBF4 to obtain a compound 4; enabling reaction of the compound 4 and 2-methylethyl acetoacetate to obtain a compound 5; treating the compound 5 with formic acid to obtain a compound 6; carrying out amid catalysis and exchange with the ionic liquid on the compound 6 to obtain a compound 7; enabling reaction of the compound 7 and 2-oxodimethyl glutaconate to obtain a compound 8; feeding hydrogen chloride to the compound 8 under the action of Cu(OAc)2*2H2O to obtain a compound 9; carrying out basic hydrolysis on the compound 9 to obtain a compound 10. The synthetic method disclosed by the invention is cheap and accessible in raw materials, stable, high in reaction yield, quick in reaction, and easy for product separation, and is environment-friendly as the catalyst can be recycled.

The invention relates to a water-soluble fertilizer for preventing fruit cracking of fruit trees. The water-soluble fertilizer comprises the following effective components: 0.2 parts of gibberellin GA3, 0.5 parts of polyglutamic acid, 8-10 parts of N, 10-13 parts of P2O5, 30-32 parts of K2O, 2-3 parts of Ca, 0.1-0.3 parts of Fe, 0.2-0.3 parts of B, 0.1-0.3 parts of Cu, and 0.1-0.3 parts of Mn; the N is provided by one or more of urea, monoammonium phosphate, potassium nitrate and calcium nitrate, P2O5 is provided by one or two of potassium dihydrogen phosphate and monoammonium phosphate, K2O is provided by potassium nitrate and potassium dihydrogen phosphate, Fe is provided by ferrous sulphate, Zn is provided by zinc sulfate, B is provided by boric acid, Cu is provided by copper sulphate, Ca is provided by calcium nitrate, and Mn is provided by manganese sulfate. The water-soluble fertilizer can enhance the fruit tree resistance performance, increases the output, increases the quality, and prevents the fruit cracking.

The invention discloses a yield-increasing water retention fertilizer special for hickory nuts. The fertilizer is prepared from, by weight, 50-150 parts of organic fertilizer, 5-15 parts of steel slag, 5-15 parts of urea, 15-25 parts of diammonium phosphate, 5-10 parts of ammonium bicarbonate, 3-15 parts of potassium sulfate, 2-10 parts of magnesium sulfate, 10-20 parts of calcium cyanamide, 3-10 parts of calcium sulfate, 1-10 parts of calcium oxide, 4-8 parts of microelements, 0.1-1 part of gamma-polyglutamic acid, 0.3-1.5 parts of vermiculite powder, 0.5-1.5 parts of bentonite, 5-15 parts of ardealite, 0.05-0.3 part of malic acid, 0.1-0.5 part of phosphate solubilizing bacteria, 0.5-3 parts of glucose, 2-5 parts of sodium potassium tartrate tetrahydrate, 2-5 parts of rare-earth salt and 1-5 parts of water-retaining agent. The yield-increasing water retention fertilizer special for the hickory nuts is reasonable in formula, comprehensive and balanced in nutrition, high in water retaining ability and capable of increasing the yield of the hickory nuts, improving quality and improving physical and chemical properties of soil.

The invention relates to an efficient high-concentration sulfur-based compound fertilizer containing poly-gamma-glutamic acid, which is prepared from urea, phosphoric acid, potassium chloride, potassium sulfate, sulfuric acid, gas ammonia and poly-gamma-glutamic acid, and also comprises a water-retaining agent. A production process of the efficient high-concentration sulfur-based compound fertilizer comprises the steps of: A, preparing a mixed acid; B, neutralizing; C, pelleting and forming; D, preparing monoammonium phosphate; E, supplementing potassium; and F, supplementing nitrogen. The invention has the advantage of being capable of manufacturing the efficient high-concentration sulfur-based compound fertilizer containing the poly-gamma-glutamic acid, with the proportion of N:P:K of 17:17:17. Meanwhile, a poly-gamma-glutamic acid fertilizer synergist is added in the production process and used as a fertilizer absorbing promoting agent used on single nitrogen or phosphorus or potassium or the combination of the nitrogen and the phosphorus as well as the potassium. In addition, the water-remaining agent is added for increasing the water-retaining effect.

The invention discloses a preparation method for fluorescent wavelength adjustable nitrogen and sulphur-co-doped carbon quantum dots, and belongs to the technical field of carbon quantum dots. The preparation method comprises the following steps: grinding and uniformly mixing L-glutamic acid and methionine in an agateware in a certain proportion; tilling the mixture at the bottom of a beaker, thenheating to 200 to 300 DEG C at a constant speed, and heating and reacting for 5 to 20 minutes in the temperature range to obtain a reaction product A; cooling the reaction product A to a room temperature; adding a passivating agent into the reaction product A, and uniformly mixing to obtain a mixed solution B; heating to enable the mixed solution B to react for 2 to 10 minutes at 200 to 300 DEG Cto obtain a mixed solution C; cooling the mixed solution C to a room temperature; performing centrifugal treatment; and standing, and dialysing through a dialysis bag to remove unreacted raw materials and impurities to obtain the nitrogen and sulphur-co-doped carbon quantum dots. The preparation process disclosed by the invention is simple and controllable; the fluorescent wavelength of the carbon quantum dots can be regulated and controlled by changing preparation conditions or the passivating agent so as to cover the wavebands of green light, yellow light and red light to meet actual application requirements.

The invention relates to a three-arm star hydrophilic copolymer, and a synthesis method and application thereof. The synthesis method comprises the following steps: initiating gamma-benzyl-L-glutamate-N-carboxy-alpha-amino acid anhydride ring-opening polymerization reaction by using a three-element primary amine inner core, and bonding small-molecule RAFT polymeric chain transfer agent to three terminated amino groups of the star polymer through a carbodiimide method, thus obtaining large-molecule RAFT chain transfer agent; and performing RAFT polymerization by using N-(3-dimethylaminopropyl) and N-hydroxymethyl acrylamide as monomers, finally reacting the hydroxyl group of the N-hydroxymethyl acrylamide component in the copolymer with isocyanated methyl-terminated polyethyleneglycol to realize connection to the polyethyleneglycol via a disulfide bond, and performing hydrazinolysis treatment to obtain the required three-arm star hydrophilic copolymer. According to the method, the molecular weight and chain length of each polymer component can be flexibly controlled, the reaction conditions are mild, and the raw materials are accessible; the synthesized polymer can improve the drug effect and reduce the toxic or side effect; and meanwhile, when loading amycin and gene-based drugs, the polymer realizes the synergic antitumor treatment effect.

The invention discloses a preparation auxiliary agent of volatile oil obtained by extracting traditional Chinese medicine, which relates to the technical field of a traditional Chinese medicine extract product preparation. The preparation auxiliary agent comprises the following raw materials in parts by weight: 10-15 parts of poloxamer / polyglutamic acid, 3-5 parts of microcrystalline cellulose, 1-3 parts of pregelatinized hydroxypropyl starch / citric acid, 0.5-1 part of sorbitol, and 0.5-1 part of hydrogenated palm oil. The prepared preparation auxiliary agent is used for inclusion of the volatile oil obtained by extracting traditional Chinese medicine, the instant inclusion rate after inclusion can reach 90% and above, the inclusion rate of the preparation after 6 months can reach 85% and above, and the inclusion rate of the preparation after 12 months can reach 80% and the above.

Polyglutamates are well known to be highly biocompatible, biodegradable and multifunctional polymers, which have been already used as building blocks in polymer drug conjugates and polymeric micelles. Those systems have been applied to various medical applications ranging from therapy to molecular imaging. Furthermore a polyglutamic acid (PGA) paclitaxel conjugate has already entered clinical studies (Opaxio™ PGA-PTX conjugate currently in phase III of Clinical trials).In this context, a synthetic pathway to a plethora functional polyglutamates (homopolymers, block-co-polymers, triblocks) with well-defined structure, adjustable molecular weight (Mw) and low dispersity (D=Mw / Mn<1.2) applying the ring opening polymerization (ROP) of N-carboxyanhydrides (NCA) has been developed. Additionally, the acid moieties of the polyglutamates can be activated with 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium (DMTMM) and various functionalities can be easily introduced by “post-polymerization modification” yielding a set orthogonal reactive attachment sides. The reactive moieties, such as azides, maleimides, thiols, alkynes (linear or cyclic) offer the opportunity of specific conjugation of the drugs, targeting moieties or markers. Besides introducing reactive groups the functionalization strategy was also used for PEGylation of PGA reducing charge induced interactions and therefore pharmacological properties, such as blood circulation time may be adjusted.In summary, a tool kit of various polyglutamates has been developed enabling the synthesis of a variety of polymer drug conjugates or polymer based imaging agents. The functional polymeric precursors developed will allow us to functionalize and therefore adjust the polymer properties to a desired application.

The invention discloses a full nutritional functional type polymer coated type strawberry fertilizer. The full nutritional functional type polymer coated type strawberry fertilizer is prepared from the following raw materials in parts by weight: 20-24 parts of urea, 0.5-1.0 part of choline chloride, 1-2 parts of nicotinic acid, 35-39 parts of fruit residue, 1-2 parts of ferroboron, 20-26 parts of silk reeling concentration liquid waste, 2-3 parts of sericite powder, 16-25 parts of dipotassium phosphate, 2-3 parts of polyglutamic acid, 0.2-0.5 part of acrylic acid, 6-9 parts of an EM (Effective Microorganisms) bacterial agent, 12-15 parts of modified bamboo fiber, 3-4 parts of diatomaceous earth, 2-4 parts of nano carbon, 2-3 parts of zinc sulfate, 2-4 parts of polyvinyl alcohol, 0.1-0.3 part of ammonium superphosphate, 0.2-0.5 part of alkylphenol ethoxylates, 0.2-0.6 part of ammonium acrylate, 4-6 parts of hydroxymethyl methacrylate, 1-2 parts of butyl acrylate, and a proper amount of water. The fertilizer disclosed by the invention does not pollute the environment and soil, increases disease resistance of crops and promotes the nutrient absorbing function of the crops.

The present invention relates to a novel method for the biocatalytic production of unsaturated dicarboxylic acids by cultivating a recombinant microorganism co-expressing a glutaconate CoA-transferase and a 2-hydroxyglutaryl-CoA dehydratase system. The present invention also relates to corresponding recombinant hosts, recombinant vectors, expression cassettes and nucleic acids suitable for preparing such hosts as well as a method of preparing polyamide or polyester copolymers making use of said dicarboxylic acids as obtained by said biocatalytic production method.

The present invention relates to a composition for coating keratin fibres, more particularly the eyelashes, characterized in that it is present in the form of a wax-in-water emulsion comprising a combination of at least one glutamic acid derivative and / or salt thereof and at least one alkylpolyglycoside.

The invention relates to a preparation method and application of a multifunctional super-sensitive Zn<2+> two-photon detection fluorescence molecular probe. Firstly, 2,4-dihydroxy benzaldehyde, diethyl glutaconate and anhydrous piperidine react in ethanol to obtain a product 1; the product 1 and acetic anhydride react in anhydrous pyridine to obtain a product 2; the product 2, osmium tetroxide andsodium periodate react in tetrahydrofuran to obtain a product 3; the product 3 and anhydrous potassium carbonate react in methyl alcohol to obtain a product 4; finally, the product 4 id dissolved into the ethanol; 2-hydrazinopyridine and glacial acetic acid are added; the steps of backflow, recrystallization and the like are performed; the multifunctional super-sensitive Zn<2+> two-photon detection fluorescence molecular probe is obtained. The probe is applicable to the qualitative and quantitative analysis of Zn<2+> in a biological sample; the detection is sensitive, accurate and fast; the probe can be applied to the relevant fields of analytical chemistry, life organic analytical chemistry, disease advanced diagnosis, medical clinic detection and the like.

The invention discloses a butyryl glutamic acid derivative as well as a composition and application thereof. The butyryl glutamic acid derivative disclosed by the invention or a racemic modification,stereisomer, geometric isomer, tautomer and solvate or feed-acceptable salt thereof can be applied in the preparation of novel feed additives and feeds. The invention further discloses a feed composition of the butyryl glutamic acid derivative or the racemic modification, the stereisomer, the geometric isomer, the tautomer and the solvate or the feed-acceptable salt thereof. When applied in animalhusbandry, the butyryl glutamic acid derivative provided by the invention has the effect of improving the production performance of animals, such as increasing animal weight increasing rate, decreasing feed conversion ratio and controlling diarrhea rate, and can be applied as an effective, safe novel feed additive.

The invention discloses an organic-inorganic compound fertilizer master batch containing gamma-polyglutamic acid and nucleotide. The organic-inorganic compound fertilizer master batch contains the following components: polyglutamic acid, nucleotide and nitrogen-phosphorus-potassium compound fertilizer, and is prepared according to a certain ratio, wherein the content of polyglutamic acid is 0.05-2% of the mass of the nitrogen-phosphorus-potassium compound fertilizer, the content of nucleotide is 1-5% of the nitrogen-phosphorus-potassium compound fertilizer, and the total organic content is more than or equal to 15%. By adjusting the ratio between polyglutamic acid and nucleotide, the release cycle of the compound fertilizer can be controlled, and the utilization rate of the fertilizer canbe effectively improved. In addition, besides nucleotide, a fermented nucleotide thallus wall breaking extraction concentrated solution is also rich in nutritional ingredients such as amino acid and vitamin, and these ingredients, as biostimulants, can also improve the growth promoting effect of the fertilizer to crops. The organic-inorganic compound fertilizer master batch containing gamma-polyglutamic acid and nucleotide can remarkably increase the crop yield, and effectively improve soil hardening caused by fertilizer application.

A special-purpose organic fertilizer for green tea planting is prepared from the following components in part by weight: 50 parts of farm manure, 15 parts of surface dust, 5 parts of concrete, 2 parts of compound sodium nitrophenolate, 12 parts of rice hulls, 5 parts of saw powder, 2 parts of gibberellin, 2 parts of sea mud, 5 parts of glutinous rice bran, 10 parts of wine stillage, 5 parts of lecithin powder, 10 parts of cottonseed meal, 5 parts of moss, 5 parts of tea dregs, 5 parts of calcium peroxide, 1.5 parts of benzoic acid, 1 parts of brassin, 1.5 parts of saponin, 0.5 part of naphthylacetic acid, 2 parts of raw starch-digesting gluconamylase, 0.5 parts of L-glumatic acid, 0.1 part of potassium sorbate, 1.5 parts of fungicide, 2 parts of se-yeast and 100 parts of spring water. During preparation, the components are mixed and stirred uniformly, are placed in a fermenting tank, and are fermented in a sealed manner for 100 days. After being fermented for 100 days, raw materials are stirred, aired and granulated. Requirements on nutrition are met, quality is improved, and the purpose of increasing both production and income is achieved.

The invention relates to L-glutamic acid terminated polypeptide MIP (molecular imprinting polymer) magnetic microspheres as well as a preparation method thereof. The preparation method comprises stepsas follows: a multifunctional magnetic CuFeMnO4 nano affine material is synthesized with a hydrothermal method, the strong coordination effect of Cu<2+> and Fe<3+> in the affine material with carboxyl and amino in polypeptide is used, the affine material serves as a carrier, alternative template molecules, functional monomers, an RAFT reagent, a crosslinking agent and an initiator are added to awater-phase system, molecular imprinting is performed on the surface of the CuFeMnO4 nano material with a one-step method, and MIPs@CuFeMnO4 microspheres are obtained after an RAFT polymerization reaction; and alternative template molecules embedded in the polymer are removed through elution, and the MIPs@CuFeMnO4 microspheres with MIP rigid identification holes are obtained. The MIPs@CuFeMnO4 magnetic affine nano-microspheres prepared with the method have the advantages of uniform surface coating, narrower imprinting polymer molecular weight distribution, stable extraction performance, high extraction selectivity and the like.

A compound having the formulaor a pharmaceutically acceptable salt thereof whereinR is hydrogen or hydroxy;R<1 >is hydrogen,alkyl,arylalkyl,(CH2)nOH, or(CH2)nNR<7>R<8>;R<5 >and R<6 >are each independentlyhydrogen,halogen,NO2,CN,CF3,SO2NR<7>R<8>,PO3R<9>R<10>,alkyl,alkenyl,alkynyl,(CH2)nCONR<7>R<8>,(CH2)nCO2R<10>,NHCOR<11>,A is a ring formed by the following:a-NR<12>-CHR<13>-CHR<14>-b,a-CHR<13>-CHR<14>-NR<12>-b,a-CHR<13>-NR<12>-CHR<14>-b,a-CHR<14>-CH2-NR<12>-CHR<13>-b,a-CHR<13>-NR<12>-CH2-CHR<14>-b,a-CH2-CH2-CHR<13>-NR<12>-b,a-NR<12>-CHR<13>-CHR<12>-CH2-CH2-b,a-CH2-CH2-NR<12>-CH2-CH2-b,a-CH2-CH2-CH2NR<12>-CH2-b,a-CH2-NR<12>-CH2-CH2-ba-CH2-CH2-CH2-CH2-NR<12>-b,a-NR<12>-CH2-CH2-CH2-CH2-b,The compounds are useful in the treatment of disorders responsive to the blockade of glutamic and aspartic acid receptors.

The invention belongs to the technical field of fine chemical synthesis, and relates to a method for synthesizing a pentene dianhydride compound by using carbon dioxide. The method comprises the following steps: using a 2-butenoic acid derivative as a raw material; adding an organic alkali and a reaction solvent, introducing carbon dioxide, stirring at 0-50 DEG C to react for 0.5-24 hours, standing to room temperature after the reaction is finished, slowly releasing unreacted gas, directly concentrating the reaction solution under reduced pressure to obtain a crude product, and carrying out column chromatography or recrystallization purification to obtain the pentene dianhydride product. According to the method, the 2-butenoic acid derivative and carbon dioxide which are cheap and easily available are used as raw materials, organic alkali is used as an accelerant, and the method is safe and simple to operate, low in toxicity and environment-friendly and has potential application valuein fine organic synthesis of medicines, pesticides and the like.

The invention relates to an amino acid protective group and particularly relates to a purified Fmoc (SO3H) protected amino acid having excellent hydrophilicity and a preparation method thereof. A main structure of the Fmoc (SO3H) protected amino acid is represented as the chemical formula II, wherein R is the side chains of alanine (Ala), valine (Val), leucine (Leu), isoleucine (Ile), proline (Pro), phenylalanine (Phe), tryptophan (Trp), methionine (Met), glycine (Gly), serine (Ser), threonine (Thr), cysteine (Cys), tyrosine (Tyr), asparagines (Asn), glutamine (Gln), lysine (Lys), arginine (Arg), histidine (His), aspartic acid (Asp) or glutamic acid (Glu).

The invention discloses a synthesization technique for a ceftibuten side chain. Adopting 2-aminothiazole acetic acid as starting material, the technique synthesizes a target compound, i.e. the ceftibuten side chain: (Z / E)-2-[2-[[( benzyloxy)formacyl]amino]-4-thiazolyl]-2-glutaconate-5-(3-methyl-2-butylene)ester by carboxyl group protection, amino group protection, hydroxymethylation, witing reaction and monoesterification. Since the invention does not use the expensive imported reagent, methyl 3-methoxyacrylate, the cost is reduced, and the invention solves the problem that industrialized material is difficultly obtained; because diphenyldiazomethane is not used, the two high-toxic and flammable chemical materials, i.e. yellow mercury oxide and diethyl ether, are not used; high-corrosive trifluoroacetic acid is not used for single hydrolysis, environment pollution is reduced, the operation of the technique is simple, controllability is high, the yield is high and stable, and the technique is suitable for industrialized production.

This invention relates to a pharmaceutical composition for oral administration comprising 4-((1-methylpyrrol-2-yl)-carbonyl)-N-(4-(4-morpholin-1-yl-carbonylpiperidin-1-yl)-phenyl)-1-piperazinecarboxamide, a salt thereof, or a solvate thereof, as an active pharmaceutical ingredient; and at least one acid additive selected from the group consisting of adipic acid, succinic acid, fumaric acid, L-aspartic acid, and L-glutamic acid.

The invention discloses a preparation method of a pyridine pyrimidine derivative. The preparation method comprises following steps: 3-methyl-2-glutaconate diester and cyclopentamine are subjected to amidation condensation to prepare 1-cyclopentyl-4-methylpyridine-2, 6-(1H, 5H)-dione, and one-pot condensation with methylation reagent (N, N-dimethylformamide acetal) and urea is carried out so as toobtain 2-hydroxyl-5-methyl-8-cyclopentyl pyridine [2, 3-d] pyrimidine-8-hydro-7-one; and then chlorination and bromination reaction are carried out to prepare 2-chlor-5-methyl-6-bromo-8-cyclopentyl pyridine [2, 3-d] pyrimidine-8-hydro-7-one. The preparation method possesses following advantages: using of expensive trihalogen pyrimidine, palladium salt catalyst, and 3-borate substituted ethyl crotonate is avoided; the adopted raw materials are cheap and easily available; operation is convenient; reaction yield is stable; less three wastes are generated; reaction atom economical benefit is high;cost is low; and the preparation method is convenient for green industrialized production.

The invention relates to a preparation method and an application of a double-rate-type (ultraviolet / fluorescence) multifunctional (calorimetric / fluorescence / ultraviolet) high-sensitivity florescent probe for carboxylesterase detection. Firstly, 2,4-dihydroxybenzaldehyde, diethyl glutaconate and anhydrous piperidine react in ethyl alcohol to produce a product 1, the product 1 and acetic anhydride react in anhydrous pyridine to produce a product 2, the product 2 reacts with osmium tetroxide and sodium periodate in tetrahydrofuran to produce a product 3, and the product 3 reacts with anhydrous potassium carbonate in methyl alcohol to produce a product 4; then methylpyridine and methyl iodide react in absolute ether to produce a product 5; next, the product 4 and the product 5 are dissolved in absolute ethanol, piperidine is added for a reaction, and a product 6 is obtained; finally, the product 6 is dissolved in acetic anhydride, anhydrous sodium acetate is added, and the double-rate-type multifunctional florescent probe for carboxylesterase detection is obtained. The probe is applicable to qualitative and quantitative analysis of carboxylesterase in biological samples, is sensitive, accurate and quick in detection, and can be applied to related fields of analytical chemistry, life organic analytical chemistry, disease pre-diagnosis, clinical medical examination and the like.

The invention provides an application of dicarboxylic acid and ester compounds thereof and in particular relates to an application of the compounds to preparation of neuroprotective drugs. In a chemical formula in the specification, R1 is hydrogen or methyl; R2 is isopropyl or isobutyl; R3 is carboxyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl, borneol oxycarbonyl or 5-tetrazole; a is 0 or 1; b is 0 or 1; c is an integer from 1 to 4; b is 0 when a is 0; b is 0 or 1 when a is 1. The compounds have relatively strong protective effects on glutamate-induced neuron damages.

The present application describes compositions and methods for producing oxidoreductases for enantioselective reactions. The present application describes compositions and methods for producing novel variants of (R)-2-hydroxyacid dehydrogenases capable of enzymatically converting 1-carboxy-2-ketoacids into 1-carboxy-( R)‑2‑hydroxy acid, or its reverse reaction. Illustrative examples include (a) (R)-2-hydroxyadipate dehydrogenase and its use for converting 2-oxoadipate to (R)-2-hydroxyadipate or its reverse reaction and (b) (R)-2-hydroxyglutarate dehydrogenase and its use for converting 2-oxoglutarate into (R)-2-hydroxyglutarate or its reverse reaction. The present application also describes methods for producing unnatural microbial organisms to enzymatically convert 2-oxoadipate to (E)-2-hexenedioic acid or adipate, or to enzymatically convert 2-oxopentanedioate Compositions and methods for the conversion of diacids to (E)-2-glutaconate or glutaric acid or the reverse reaction of each.