711 results about "Total synthesis" patented technology

The present invention relates generally to the fields of oligonucleotide synthesis. More particularly, it concerns the assembly of genes and genomes of completely synthetic artificial organisms. Thus, the present invention outlines a novel approach to utilizing the results of genomic sequence information by computer directed gene synthesis based on computing on the human genome database. Specifically, the present invention contemplates and describes the chemical synthesis and resynthesis of genes defined by the genome sequence in a host vector and transfer and expression of these sequences into suitable hosts.

The invention discloses a water-soluble total-synthesis metal working fluid and application thereof. The working fluid is prepared from the following raw materials in percentage by weight: 1wt%-30wt% of a lubricant, 1wt%-40wt% of a corrosion inhibitor, 1wt%-40wt% of organic amine, 1wt%-20wt% of a cleaning agent, 1wt%-20wt% of a coupling agent, 0.5wt%-5wt% of an antifoaming agent and the balance of water. The working fluid can form water-based steam with anti-rust property in an induction manner in the use procedure, so that the problem of rusting caused by steam which is easily generated by a closed machine tool is solved, and therefore, the working fluid is suitable for a high-precision machine tool, especially a numerical control machine tool with a closed structure.

The present invention is to prepare efficiently 2′-amino-5′-hydroxypropiophenone corresponding to the AB-ring part of camptothecin (CPT) skeleton and a tricyclic ketone corresponding to the CDE-ring part in order to provide efficiently CPT by the total synthesis, which is a starting material for irinotecan hydrochloride and various kinds of camptothecin derivatives, and to provide stably CPT and its derivatives.

The invention discloses a fully synthetic cutting fluid which comprises anion active agent, non-ionic surface active agent, polyethylene glycol, borax, bactericide, foam suppressor, pH regulator, water and additive; wherein, the additive is prepared by the following method: the surface active agents are dissolved by acetone, the mixed solution is added with toluene and heated up to 50-60 DEG C, and the reaction system is dripped with acrylate monomer as well as azodiisobutyronitrile (AIBN) or ammonium persulfate (APS) evocating agent; after that, the temperature is preserved for 3-5h, the reaction stops, and organic solvent is removed, so that the additive is obtained. Compared with the existing fully synthetic cutting fluid, the fully synthetic cutting fluid of the invention can completely inhibit leaching of cobalt element in hard alloy containing cobalt when metal is processed, well solves the problem of separating the cobalt in the existing fully synthetic cutting fluid, and is environment-friendly and efficient.

The invention belongs to the field of metal machining fluids, and discloses a heavy-load metal machining total synthesis cutting fluid as well as a preparation method and an application thereof. The total synthesis cutting fluid comprises the following components in percentage by weight: 20%-30% of mixed alcohol amine, 6%-9% of anti-rust agents, 4%-6% of special amine, 6%-10% of lubricating agents, 15%-25% of extreme pressure agents, 6%-10% of cosolvents, 1%-2% of water-softening agents, 1%-3% of corrosion inhibitors and the balance of water. The total synthesis cutting fluid disclosed by the invention has excellent lubricating extreme pressure property, can meet the requirement for heavy-load machining, namely reaming, drilling, tapping, threading, broaching, thread machining and the like, of difficult-to-machine materials, namely high-temperature alloy steel, a titanium alloy and the like; a product is green and environment-friendly without containing boron, sodium nitrite, secondary amine, chlorine, phenol, formaldehyde, heavy metals and the like; in addition, the total synthesis cutting fluid disclosed by the invention has excellent anti-rust property, biological stability and machining property, and can enhance the surface quality of a machined part, prolong the service life of a cutter and reduce the rejection rate, thus improving the production efficiency.

A simple and effective stereocontrolled synthesis of salinosporamide A(1)has been developed which follows the pathway outlined in the FIGURE. The process, the first total synthesis of salinosporamide A, is capable of providing the compound in substantial quantities for further biological studies. In addition to the method of Scheme I, the present invention also includes several novel synthetic intermediate compounds, several intermediate steps of the preferred synthetic process; and the uses of these compounds in the preparation of synthetic derivatives of the compound Salinosporamide A. Salinosporamide A is of special interest as a synthetic target because of its protein in vitro cytotoxic activity against many tumor cell lines (IC50 values of 10 nM or less).

The invention provides a total synthesis method for preparing the icariin compound with a structural formular as (I); R<1> symbolizes H or Rham and R<2> symbolizes H or Glc. By adopting the Claisen rearrangement reaction triggered by the microwave, the method leads the isopenteny in with positioning on the flavone ring with high selectivity so as to enhance the overall yield and lead to the easily obtained raw materials and higher yield of the icariin compound. The invention is suitable for industrialized production and solves the problem that the compound can be only prepared through extraction and separation in the Chinese herbal medicine extractum with extremely low efficiency.

Provided are worm-like micelles, capable of encapsulating at least one encapsulant, wherein each worm-like micelle comprises one or more wholly synthetic, polymeric, super-amphiphilic molecules that self assemble in aqueous solution, without organic solvent or post assembly polymerization; and wherein at least one of said super-amphiphilic molecules is a hydrophilic block copolymer, the weight fraction (w) of which, relative to total copolymer molecular weight, directs assembly of the amphiphilic molecules into the worm-like micelle of up to one or more microns in length, and determines its stability, flexibility and convective responsiveness. Also provide are methods of preparing and methods of using the worm-like micelles, particularly when loaded with one or more encapsulants. The loaded worm-like micelles of the present invention are particularly suited for the stable and controlled transport, delivery and storage of materials, either in vivo or in vitro.

The present invention relates to novel biologically active compounds from fungi of the species Ganoderma pfeifferi DSM 13239, processes for their preparation, and their use. From the fruit body and mycelium of the species Ganoderma pfeifferi DSM 13239, extracts can be obtained which have antimicrobial activity and are suitable as preserving agents, for pharmaceutical and cosmetic preparations, for controlling infections, and for use in fish breeding. Antimicrobially active substances called ganomycins having activity against multiresistant germs are isolated from the extracts. The total synthesis of the ganomycins and their derivatization enables their use an antibiotics.

Procedure for the synthesis of deprotected pentasaccharides from a protected precursor pentasaccharide through a reaction procedure having five stages whereamong is included an N-sulphation of amino groups and a hydrogenolysis of benzyl groups. Through this procedure a drastic reduction is achieved in the total synthesis time in comparison with the process traditionally employed, together with increased reproducibility thereof, permitting the standardisation thereof.

The invention discloses complete synthesis cutting fluid capable of meeting machining requirements of multiple materials, prepared from the following components in percentage by weight: 10-25 percent of organic alcohol amine, 5-15 percent of antirust agent, 5-15 percent of extreme-pressure lubricant, 0-2 percent of water softener, 0-2 percent of aluminium corrosion inhibitor, 0.1-1 percent of copper corrosion inhibitor, 0-4 percent of cosolvent, 0.5-4 percent of bactericide, 0.1-1 percent of mildew preventive, 0.1-0.5 percent of defoamer and the balance of water. The complete synthesis cutting fluid can meet the machining requirements of workpieces made of multiple materials such as black metal, aluminium alloy, copper alloy and hard alloy; meanwhile, the cutting fluid has good lubricating property, can be used for machining of various types, such as grinding, milling, turning, light-medium load tapping and drilling; the complete synthesis cutting fluid is good in rust-proof and anticorrosion properties, can meet storage requirements among work procedures, and all components in a formula are green, environment-friendly, free of stimulation to a human body, and low in smell.

[Problems to be Solved]To provide an effective process for total synthesis of pladienolide B and pladienolide D having excellent anti-tumor activity and to provide useful intermediates in the above-described process. [Measure for Solving the Problem]A process for producing a compound represented by Formula (11): wherein P1, P7, P8, P9 and R1 are the same as defined below, characterized by including reacting a compound represented by Formula (12): wherein P7 means a hydrogen atom or a protecting group for hydroxy group; R1 means a hydrogen atom or a hydroxy group, with a compound represented by Formula (13): wherein P1 means a hydrogen atom or a protecting group for hydroxy group; P8 means a hydrogen atom, an acetyl group or a protecting group for hydroxy group; P9 means a hydrogen atom or a protecting group for hydroxy group; or P8 and P9 may form together a group represented by a formula: wherein R5 means a phenyl group which may have a substituent, in the presence of a catalyst.

This invention relates generally to methods for synthesizing the non-addictive alkaloid noribogaine.

The invention relates to an anti-human TIGIT monoclonal antibody which is particularly related to high-affinity anti-human TIGIT monoclonal antibody with blocking activity. A large-capacity fully-synthetic human phage antibody library is constructed, the specific anti-human TIGIT monoclonal antibody and the high-affinity anti-human TIGIT monoclonal antibody which is optimized after molecular evolution are screened from the human phage antibody library, and the monoclonal antibody comprises a full-human frame region and variable regions of a full-human light chain and a heavy chain.

The present invention is to prepare efficiently 2'-amino-5'-hydroxypropiophenone corresponding to the AB-ring part of camptothecin (CPT) skeleton and a tricyclic ketone corresponding to the CDE-ring part in order to provide efficiently CPT by the total synthesis, which is a starting material for irinotecan hydrochloride and various kinds of camptothecin derivatives, and to provide stably CPT and its derivatives.

The invention provides a human anti-vascular endothelial cell growth factor (VEGF) antibody as well as a coding gene and an application thereof. According to the invention, by virtue of genetic engineering means and a phage surface display technology, an anti-VEGF genetic engineering single-chain antibody is screened from a complete synthesis single-chain human antibody library, a variable region gene sequence of the anti-VEGF genetic engineering single-chain antibody is obtained, amino acids in a CDR (complementary determining region) of the anti-VEGF genetic engineering single-chain antibody are transformed by virtue of bioinformatics means, and finally a series of high-affinity anti-VEGF antibodies are obtained by constructing and screening mutation libraries and utilizing a chain exchange method, wherein affinity of the anti-VEGF antibodies with human VEGF is 10<-9>-10<-11>M. According to the invention, identification on immunocompetence and biological activity of the antibody is completed, the anti-VEGF antibody is verified to have the characteristic of being antagonistic to combination of VEGF and VEGFR2 and can effectively inhibit proliferation of vascular endothelial cells induced by VEGF. The invention provides a new specific candidate antibody molecule for resisting tumour and senile macular degeneration targeted by VEGF in future.

The invention discloses a composite extreme pressure anti-wear agent and total-synthesis anti-wear hydraulic oil containing the composite extreme pressure anti-wear agent, belonging to the field of production of lubricating oil. The hydraulic oil is mainly prepared by mixing aqueous base oil and the composite extreme pressure anti-wear agent, wherein the composite extreme pressure anti-wear agent is a compound of two kinds of imidazolyl tetrafluoroborate ion liquid. Compared with the prior art, the total-synthesis anti-wear hydraulic oil has the characteristics of excellent lubricating performance, energy saving, environment friendliness and the like and has high popularization and application values.

The invention belongs to the field of chemical synthesis, in particular relates to a synthesis method of a natural product mangostin which is shown in the formula (I) and has good anti-tumor activity, anti-inflammation activity and anti-bacterial activity. The method provided by the invention comprises the following steps of: taking 2,4,5-trialkoxy benzoic acid and 1,3,5-trialkoxy benzene as initial raw materials; carrying out acyl chlorination, Friedel-Crafts acylation and cyclization to prepare a key intermediate 1,3,6,7-tetraalkoxy xanthone; and then, carrying out dealkylation, allylation, Claisen rearrangement, methylation, oxidation reaction, WITTING reaction and dealkylation reaction so as to prepare the mangostin.

The invention relates to a preparation method of DHA (which relates to an unsaturated fatty acid. The invention provides a preparation method of a fully synthetic medium that is suitable for high density growth of fissiparism chytrid and increases the output of the DHA. The DHA comprises a carbon source, amino acids, lysine, inorganic salts, vitamins, trace elements and water. The carbon source is glucose, the amino acids comprise alanine, methionine, cysteine, lysine, histidine, glutamic acid, glutamine, isoleucine, threonine and tryptophan; the vitamins comprise VB1, VB12, biotin, lipoic acid and folic acid; the inorganic salts comprise NaCl, KCl, MgCl2, CaCl2, Na2HPO4 and KH2PO4; and the trace elements comprise AlCl3, H3BO3, ZnSO4, MnCl2, CuSO4, FeSO4 and (NH4)6Mo7O24.4H2O. The synthetic medium is utilized for culturing the fissiparism chytrid based on a shake flask, and the output of the DHA is 9.8g / L.

The present invention relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs from a compound of formula (V).

The invention provides total-synthesis water-based cutting fluid for sapphire and a preparation method of the cutting fluid. The cutting fluid for the sapphire comprises the following components of: in percent by weight, 8-25% of lubricant, 2-10% of rust inhibitor, 2-7% of an extreme-pressure additive, 0.25-2% of a settling agent, 0.5-3% of fungicide, 0.2-0.8% of a wetting agent, 3-5% of a cosolvent, 4-15% of pH stabilizer, 0.2-0.8% of defoamer and the balance water. According to the total-synthesis water-based cutting fluid for the sapphire, the reasonable additives are adopted for compounding, lubricating and wetting permeation performance of the cutting fluid are better than common water-based cutting fluid for sapphire, the total-synthesis water-based cutting fluid for the sapphire canreach the level of oil-based cutting fluid for the sapphire, and meanwhile the defects of poor powder sedimentation, large oil mist, potential risks for open flames, difficult post-processing and thelike of the oil-based product are avoided.

The invention discloses a totally-synthesized water-based stainless steel cutting liquid. The cutting liquid contains the following components: a stainless steel water-based extreme-pressure agent, caprylic-capric acid, boric acid triethanolamine ester, polyethylene glycol, a cation quaternary ammonium salt metal filings settling agent, a dicarboxylic compound antirusting agent, a monobutyl ether coupling agent, a hard-water-resisting agent, a defoamer and distilled water. By virtue of an environmental-friendly total-synthesis formula, the cleaning and settling properties of the cutting liquid are enhanced; an environmental-friendly special water-based extreme-pressure lubricant is used to substitute for the traditional synthetic ester, thereby ensuring the long-time stability of the cleaning and settling properties of the cutting liquid. The cutting liquid plays a very good role in protecting non-ferrous metal and ferrous metal; by virtue of the cation quaternary ammonium salt settling agent, the problem of iron filings settling during the processing of stainless steel is eliminated, and the transparency and stability of the cutting liquid in long-time use are guaranteed.

The invention relates to a full synthetic aluminum drawing fluid composition, which comprises the following components: 5 to 20 percent of mixed alkylol amine, 5 to 15 percent of mixed acid, 0.2 to 0.8 percent of copper corrosion inhibitor, 1 to 4 percent of antirusting agent, 5 to 15 percent of hexanediol, 1 to 5 percent of aluminum corrosion inhibitor, 5 to 30 percent of water-soluble polyether, and the balance of water. The full synthetic aluminum drawing fluid composition is characterized in that: the full synthetic aluminum drawing fluid composition has excellent lubricating property, cleaning and aluminum protective property; the good lubricating property can meet the machining accuracy requirement; the good cleaning ensures that a workpiece can be quickly cleaned in the next working procedure, and does not influence the operation; and the good aluminum protective property can meet the brightness requirement of the workpiece. The drawing fluid is prepared from basic solution, sothe drawing fluid does not contain a bactericide.

The invention relates to total synthesis shock absorber oil with a high viscosity index, which comprises the following components in percentage by weight: 85-95% of poly-alpha-olefin synthetic oil, 1-10% of ester synthetic oil, 1-10% of polymethacrylate viscosity index improver, 0.1-5% of anti-wear additive, 0.5-5% of antioxidant, 0.001-0.1% of anti-foaming agent, 0-1% of pour point depressant and 0.01-2.0% of antirust additive. Compared with the common shock absorber oil, the invention has the advantages of remarkable viscosity-temperature performance and antifoaming performance, excellent low temperature performance and lubricating property, favorable antirust and anticorrosion performance, and very remarkable oxidation resistance and appropriate cost, has favorable adaptability with rubber at the same time and can satisfy the use requirements, such as all weather, long life, universality, and the like.

Disclosed is an asymmetric total-synthesis method for chiral huperzine a. The method takes 1,4-dihydro-spiro (4,5) -8 -decanone as starting material to get benzoate through hydroxymethylation and the treatment of benzoyl chloride and K2CO3; the benzoate is reacted with hydrogen sulfate O-methyl iso urea to get quinazoline; after the ketal is eliminated, Mander reagent is used for methyl esterification reaction so as to obtain beta-keto ester. Chiral ammonia, such as cinchona alkaloid, is used to promote the tandem asymmetric Michael addition / aldol condensation reaction of beta-keto esters and methyl acrolein. The compound carboxylate of diastereoisomer is reacted with MsCl, triethylamine and DMAP to get transformed. Through TMSI and MeOH processing, the protective group is removed so as to obtain optically pure-chiral huperzine a.

The invention relates to ammonia synthesis loops containing gasses, which do not react and would accumulate if they were not purged out. By the present invention ammonia in a purge gas is recovered by an adsorption agent operating at the full synthesis loop pressure. The adsorption agent is chosen in such a way that the ammonia can be removed again by passing a gas comprising hydrogen and nitrogen through it at the same elevated pressure as the loop pressure. This enables the adsorption agent to be regenerated by fresh synthesis gas coming from the synthesis gas compressor just before this gas enters the synthesis loop. Thereby, the regeneration requires an absolute minimum of energy consumption and equipment.

The invention provides a fully-synthetic water-based anti-rust complex agent, and an evaluation method and application thereof. The fully-synthetic water-based anti-rust complex agent comprises, by weight, 5-20 parts of an organic anti-rust agent, 0.2-8 parts of an inorganic anti-rust agent, 5-25 parts of an organic base and 0.005-5 parts of a lubricating anti-rust aid, with the balance being water. The fully-synthetic water-based anti-rust complex agent of the invention is green and environment-friendly, has excellent rust prevention performance, and can be used for inter-process rust prevention of ferrous metals; at the same time, the complex agent has lubricating and anti-wear properties and can be used for abrasive machining of ferrous metals.

The invention discloses a total synthesis metal cutting solution comprising the following components by weight percent: 0.5-1% of pH regulator, 10-20% of antirust agent, 10-15% of mixed hydramine, 5-8% of lubricating agent, 0.1-0.3% of copper alloy corrosion inhibitor, 1-2% of sterilizing agent, 0.1-0.2% of defoaming agent, 0-0.5% of EDTA-4 sodium and the balance of water. The invention provides a preparation method of the total synthesis metal cutting solution. The total synthesis metal cutting solution is good in lubricating performance, and the use effect is superior to that of emulsification solution. By utilizing the total synthesis metal cutting solution, surface smoothness of a workpiece can be improved, a grinding wheel can not be sticked, and abrasion of the grinding wheel is reduced. The total synthesis metal cutting solution has a good sedimentation effect and is less in bubbles, long in service life and excellent in anti-rust property, cooling property, permeability and cleanability. By utilizing the total synthesis metal cutting solution, the service life of the grinding wheel can be effectively prolonged. The total synthesis metal cutting solution is suitable for materials, such as bearing steel, carbon steel and the like, the solution is colorless and transparent, and surface processing conditions are easy to observe. Meanwhile, the total synthesis metal cutting solution does not contain toxic and harmful substances, such as sodium nitrite, phenols and the like and is harmless to environment and operator health.

The invention discloses a total-synthesis type cutting fluid which is applicable for processing cobaltic alloy material, and is composed of the following weight portions of materials: 50-70 parts of water, 8-20 parts of boric acid, 5-18 parts of special amine, 4-20 parts of common alcohol amine, 2-15 parts of synthetic fat, 5-25 parts of antirust, 0.3-1.5 parts of inhibiter, 0.1-5 parts of surfactant, 0-3 parts of addition agent. The preparing method includes the steps of adding the boric acid, the special amine and the common alcohol amine into water; stirring and fully dissolving the solution under the condition of 15-35 DEG C; and then adding in and stirring the synthetic fat, the antirust, the inhibiter, the surfactant and the addition agent fully; adjusting the PH value to 8.5-9.5 after the above substance is dissolved completely. Then the total-synthesis type cutting fluid which is applicable for processing cobaltic alloy material is produced. The total-synthesis type cutting fluid has cobalt precipitation preventing property, can settle fine abrasive dust simultaneously, has high lubricating and antirust performances, is applicable for processing manifold materials, and has long service life and excellent environment protecting performance.

The invention relates to a novel chemical synthesis method of bromphenol PTP1B inhibitor which has a chemical structural formula as follows: wherein a group connected with 2,2' and the number 3, 3' carbon of benzene ring is bromine atom; 4,4' and the number 5, 5' carbon of the benzene ring are connected with hydroxy; and the PTP1B inhibitor has a chemical name in English: Bis-(2,3-dibromo-4,5-dimethoxy-phenyl)-methane. The compound negatively regulating an insulin signal transduction path by restricting the activity of protein tyrosine phospholipase 1B and has favorable curing effect for type 2 diabetes in insulin resistance types.