19 results about "Total synthesis" patented technology

The application discloses a full synthesis method of clethodim, and the method is characterized by reasonable selection / design of a process route, simplified process flow, reduced separation and purification operation, effectively reduced production cost and improved production efficiency, further improved yield of a key intermediate through research and screening of process conditions of the key step, reduced generation of impurities, and improved product quality and yield of the target product.

This invention relates to "an efficient and safe method for synthesizing perfluoropentanone," belonging to the field of organic chemical synthesis. The method for synthesizing perfluoropentanone is characterized by the following steps: under the action of hexafluoropropylene CF2=CF-CF3, fluorophosgene CF2O, and trifluorobromomethane CF3Br, perfluoropentanone (C5F) is generated in the gas phase. 10 O. The raw materials of this invention are inexpensive and readily available; the product separation and purification are simple; it is easy to industrialize; and it produces less industrial waste.

The present application belongs to the technical field of microbiology, and particularly relates to a polypeptide for inhibiting the activity of influenza virus neuraminidase 2. The polypeptide of polyporus umbellatus is extracted, the polyporus umbellatus polypeptide is fractionated by using a Bio-Rad high-pressure chromatography system, and the polypeptide sequence with a higher inhibition rate and higher abundance is picked for full synthesis under the guidance of influenza virus neuraminidase 2 inhibition activity screening, so as to obtain a polypeptide monomer as shown in the sequence table SEQ ID NO. 1. The results of the examples show that the polypeptide monomer can effectively inhibit the activity of influenza virus neuraminidase 2, and further provides a new direction for an anti-influenza virus active substance.

This invention discloses novel cyclic tripeptide compounds from cicada molts, their preparation methods, and applications, relating to the field of pharmaceutical development technology. This invention extracts and isolates two racemic cyclic tripeptide compounds from cicada molts using methanol and ethanol-water, respectively, and then synthesizes them totally, with the following structural formulas: [structural formulas omitted]; named Pericicapeptide A (compound 1) and Pericicapeptide B (compound 2). This is the first time that novel cyclic tripeptide compounds have been isolated and identified from cicada molts, and this invention is also the first to disclose a method for extracting, isolating, and totally synthesizing the new compounds Pericicapeptide A and Pericicapeptide B from cicada molts. Structural identification confirms that these small molecule compounds are novel racemic cyclic tripeptide compounds. Experimental verification shows that they can prevent and treat neuroinflammation and depression by inhibiting the level of pro-inflammatory cytokines induced by LPS in BV2 cells.

This document discloses a method for generating intermediates in the total synthesis of (+)-daunoglobin or its derivatives, and the total synthesis of (+)-daunoglobin or its derivatives. This document also discloses methods for forming compounds of formula XIV and XV, wherein compounds of formula XIV and XV are as defined in the specification.

The invention relates to a liquid-phase synthesis method and application of 5 '-triphosphoric acid modified oligonucleotide. The liquid-phase synthesis method comprises the following steps: synthesis of 5'-terminal phosphoric acid modified oligonucleotide, ammonolysis, salting-out, activation of 5 '-terminal phosphoric acid, connection of pyrophosphoric acid and ethanol precipitation. According to the invention, a liquid phase method is creatively designed to synthesize the oligonucleotide modified by triphosphoric acid, the dependence on a solid phase carrier can be avoided, the synthesis process is safe, the synthesis efficiency is high, the application scene of the synthesis is obviously expanded, and safe, stable and cheap synthesis of the oligonucleotide modified by 5 '-triphosphoric acid is realized.

Disclosed are a method for biological total synthesis of paclitaxel key precursor substance baccatin III, a biological material and use thereof. The bioenzyme composition used in the method comprises a taxane 9α-hydroxylase (T9αH) and a taxane C4-C20 oxetanase (TOT). According to the disclosure, a core component of a baccatin III biosynthetic pathway is identified, a baccatin III artificial synthesis route is constructed, thereby paving the way for efficiently developing a green low-carbon production pathway of taxane products (such as paclitaxel) through synthetic biology.

The application discloses a kind of Δ 8 - Synthesis method and Δ 8 - Application of THC. Wherein, the synthesis method comprises the following steps: taking cannabidiol as raw material, adding organic solvent, converting under ultraviolet light to generate Δ 8 - THC. According to the technical scheme of the application, cannabidiol CBD is converted into Δ 8 - THC under the catalysis of ultraviolet light, so that Δ 8 - THC appears as main product, and the method for converting CBD also ingeniously avoids complex and high-cost total synthesis route.

This invention discloses a method for preparing the natural product mycenolide A, comprising the following steps: mixing compound 2, IBX oxidant, and solvent to carry out an oxidation reaction to obtain the natural product mycenolide A; the structural formulas of compound 2 and the natural product mycenolide A are as follows: This invention proposes and realizes for the first time an efficient total synthesis strategy for all possible chiral isomers of mycenolide A, not only solving the scientific problem of the scarcity of natural mycenolide A and its unknown absolute configuration, but also providing solid technical support and material guarantee for subsequent evaluation of neuroprotective activity and development of related original drugs due to its excellent synthetic efficiency and comprehensive coverage of chiral isomers.

This invention relates to a synthesis block for synthesizing superhard composite sheets with a diameter greater than 70 mm. The synthesis block is cuboid in shape, with the length and width being the same, ranging from 98 to 100 mm. The total height of the two separate blocks is 0.4 to 1 mm greater than the length or width, and the inner diameter is 79 to 83 mm. The synthesis block includes a sealing layer with a cavity within it. A core pillar, composed of multiple stacked blanks, is located within the cavity. The core pillar has a diameter greater than 70 mm. During synthesis, a six-sided top press is used. The top hammer has a side length of 84 to 88 mm, a small bevel angle of 41.5°, a length of 18 to 20 mm, a diameter of 240 to 260 mm, and a height of 170 to 180 mm. Using the synthesis block of this invention can effectively solve the problem of blowouts during the synthesis of large-diameter superhard composite sheets, and can safely synthesize superhard composite sheets with a diameter greater than 70 mm.

The application provides a dual-target small molecule inhibitor for treating gastric cancer and a preparation method and application thereof, the inhibitor aims to improve an anti-tumor effect by synergistically inhibiting two key signal paths in the gastric cancer, and provides a new medicinal compound for targeted treatment of the gastric cancer, meanwhile, raw material cost of the application is low, reaction conditions are mild and safe, and the synthesis route is less and the cycle is short.

The present application belongs to the technical field of microbiology, and particularly relates to a polypeptide for inhibiting the activity of influenza virus neuraminidase 2. The polypeptide of polyporus umbellatus is extracted, the polyporus umbellatus polypeptide is fractionated by using a Bio-Rad high-pressure chromatography system, and the polypeptide sequence with a higher inhibition rate and higher abundance is picked for full synthesis under the guidance of influenza virus neuraminidase 2 inhibition activity screening, so as to obtain a polypeptide monomer as shown in the sequence table SEQ ID NO. 1. The results of the examples show that the polypeptide monomer can effectively inhibit the activity of influenza virus neuraminidase 2, and further provides a new direction for an anti-influenza virus active substance.

This invention discloses benzoic acid hapten, antigen, antibody, and their preparation methods and applications, involving benzoic acid hapten, antigen, antibody, fluorescence immunochromatographic detection device, and its application in detecting benzoic acid residues. This invention prepares benzoic acid hapten and artificial antigen through a total synthesis method. This method preserves the carboxylic acid group in the benzoic acid structure, ensuring the integrity of the benzoic acid hapten, and further successfully prepares a specific antibody for detecting benzoic acid, with an IC50 value of [missing information]. 50 The effective value was 5.89 ng / mL, and the linear detection range was 1.56–22.27 ng / mL. Furthermore, the benzoic acid antibody prepared using the hapten and antigen of this invention showed cross-reactivity rates of less than 0.01% with common structural analogs, demonstrating high accuracy and effectively eliminating interference from other structural analog drugs. This provides a core reagent for establishing a rapid detection method for benzoic acid.

The application provides an asymmetric total synthesis method of alkaloid martinellic acid. Compared with the prior art, the asymmetric total synthesis method provided by the application constructs a pyrroloquinoline skeleton through a transition metal catalyst catalyzed tandem asymmetric cyclization reaction, and realizes carbon chain growth and amine group introduction through an olefin hydroamination carbonylation reaction, raw materials are simple and easy to obtain, the synthesis route is simple, and the conversion efficiency is high, so that the application provides a new idea and platform for drug molecule design and modification.

This invention relates to the field of compound preparation technology and discloses a preparation process for 3-amino-4-methoxybiphenyl salt, comprising the following steps: (1) adding 3-acetyl-4-methoxybiphenyl to solvent a, and successively adding alkali and hydroxylamine salt to carry out oxime reaction. After the reaction is completed, water is added, solvent a is recovered under reduced pressure, and after cooling, it is filtered and dried to obtain intermediate 1 dry product; (2) adding intermediate 1 to solvent b, adding catalyst, and carrying out rearrangement reaction under certain temperature conditions to obtain intermediate 2; (3) adding acid to intermediate 2 to carry out hydrolysis reaction to obtain 3-amino-4-methoxybiphenyl salt. The oxime-rearrangement-hydrolysis combined route avoids dangerous processes such as nitration and hydrogenation, and has significant advantages such as mild reaction conditions, safety and environmental protection, high yield, good product quality, and low industrialization cost, which is in line with the concept of green and safe synthesis technology.

The present application relates to a kind of full synthesis easy-to-clean copper cutting fluid and its preparation method.The raw material of the full synthesis copper cutting fluid includes composite rust inhibitor, chelating agent, special amine, aluminum copper corrosion inhibitor, lubricant, defoaming agent and solvent, and the composite rust inhibitor is composed of sebacic acid and dodecanedioic acid.The composite rust inhibitor can overcome discoloration corrosion well, has obvious cost advantage, and will not produce obvious color residue, can meet the existing user demand.Sebacic acid and dodecanedioic acid are not long carbon chain (C10 / C12) can be embedded in the gap of lubricating film, improve boundary lubrication performance, make friction coefficient reduce 5~8%, adapt to medium-low speed heavy load processing, not easy to break in long-term cyclic use (>6 months), especially suitable for the processing of nickel-containing copper alloy, can reduce the risk of pitting.

The application discloses a kind of organic total synthesis methods of nimesulide derivatives, it is obtained by the reaction of phenol derivative and nitration test, first intermediate;First intermediate and esterification reagent are esterified, and second intermediate is obtained;Second intermediate and nucleophilic reagent are substituted, and third intermediate is obtained;Third intermediate and phenol derivative are coupled, and fourth intermediate is obtained;Fourth intermediate and reducing agent are reduced, and fifth intermediate is obtained;Fifth intermediate and sulfonylation reagent are sulfonylated, and sixth intermediate is obtained;Sixth intermediate and nitration reagent are nitrified, and nimesulide derivative is obtained.The application selects more easily preserved, cheap and easily obtained and higher safety substrate and reagent, process is simple, reaction condition requirement is low, green environmental protection, safety performance is good, product yield is high, easy to scale production.

The application discloses a full synthesis method of cephinold H and fortalpinoid C, comprising the following steps: taking natural product cephanolide B as a raw material, carrying out oxidative de-arrangement and acetylation to obtain a dienone compound, then carrying out ring expansion rearrangement to obtain natural product cephinold H as a secondary product, then introducing an occupying group (Br or Cl atom) to improve the regioselectivity of the ring expansion rearrangement, so that a ring expansion product substituted with a halogen atom (Br or Cl atom) is obtained in a high proportion, then removing the halogen atom (Br or Cl atom) under a palladium catalytic reduction condition to obtain natural product cephinold H, then oxidizing cephinold H by selenium dioxide and reducing by sodium borohydride to obtain natural product fortalpinoid C with opposite configuration, and finally inverting the configuration of the hydroxyl group through a Mitsunobu reaction, so that the chemical synthesis of fortalpinoid C is realized, and the synthesis route has the advantages of simplicity, high efficiency, simple operation, low cost and the like, and is suitable for the mass synthesis of cephinold H and fortalpinoid C, and provides an important material basis for the bioactivity evaluation of the two products.