154 results about "Phosphoramides" patented technology

The invention discloses a high-molecular-weight phosphamide aggregate flame retardant and a preparation method thereof.The method comprises the steps that phosphoryl dichloride compounds and piperazine anhydrous serve as raw materials, an amino-terminated phosphamide polymer is synthesized through a condensation reaction, and the phosphamide polymer flame retardant is obtained. The high-molecular-weight phosphamide aggregate flame retardant is obtained through a ring-opening reaction of amino-terminated groups and epoxy groups between the high-molecular-weight phosphamide aggregate flame retardant and triglycidyl isocyanurate. Compared with an existing small-molecule flame retardant, the flame retardant is higher in thermal stability, better in compatibility with a high polymer material matrix, not prone to migration and capable of achieving synergistic flame retardance due to the fact that the flame retardant contains phosphorus and nitrogen structural units at the same time, and when the prepared flame retardant is added into TPU, PC, EP, PET and other transparent matrixes, the flame retardance is improved. The flame retardant property of the transparent base material can be improved, and meanwhile, good mechanical property and high light transmittance can be kept. In addition, the preparation method disclosed by the invention is simple and easy to control, high in yield, wide in source of required raw materials, easy for industrial production and wide in industrial application prospect.

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses a cyclophosphamide ternary nano-micelle and a preparation method thereof.The cyclophosphamide ternary nano-micelle prepared through the method can be used for treating malignant lymphoma, multiple myeloma, leukemia, breast cancer, ovarian cancer, cervical cancer, prostatic cancer, colon cancer, bronchial cancer, lung cancer and the like. Reasonable preparation steps and a preparation formula are adopted, the use of an organic reagent is reduced, the irritation of cyclophosphamide is reduced and the stability of the micelle is improved by adjusting a freeze-drying technology, and the cyclophosphamide micelle adopts amphiphilic macromolecules as a carrier material, so that the drug loading capacity and the stability of the micelle are obviously improved, and the bioavailability of the micelle is improved. The ternary nano-micelle system has the advantages that the solubility of cyclophosphamide is improved, the in-vivo bioavailability is increased, the preparation method is simple, the micelle performance is stable, and large-scale industrial production is facilitated.

The invention relates to the technical field of flame-retardant PC, in particular to a flame-retardant insulating PC thin film material for a battery and a preparation method of the flame-retardant insulating PC thin film material. The preparation method comprises the following steps: mechanically mixing a phosphaphenanthrene modified silicon dioxide filler, a phosphamide modified silicon dioxide filler and a biphenyl modified silicon dioxide filler to obtain a flame-retardant silicon dioxide filler; and fully mixing the polycarbonate resin, the flame-retardant silicon dioxide filler, the carbon black, the anti-dripping agent, the antioxidant and the dispersing agent, and carrying out melt blending, extrusion granulation and extrusion film forming to obtain the PC film material. The PC thin film material prepared by the invention has good flame retardance and corrosion resistance, so that the PC thin film material has a wide application prospect in the technical field of flame-retardant PC.

The invention relates to the technical field of rubber material preparation, and discloses a flame-retardant environment-friendly rubber material and a preparation method thereof. The preparation method comprises the following steps: carrying out ball milling on phosphamide bis-hexafluorophosphate ionic liquid and a carbon nanotube to obtain an ionic liquid modified carbon nanotube; and mixing with silicone rubber, a vulcanizing agent and the like, and vulcanizing to obtain the flame-retardant environment-friendly rubber material. The phosphamide bis-hexafluorophosphate ionic liquid contains a plurality of hexafluorophosphate ionic groups, and has a large interaction force with the carbon nanotubes, so the surface modification of the carbon nanotubes is effectively realized, the dispersibility of the carbon nanotubes in a silicone rubber matrix is improved, and the tensile property, hardness and other mechanical properties of the silicone rubber are improved. The ionic liquid contains phosphamide and imidazole groups to form a nitrogen-phosphorus flame retardant, and the nitrogen-phosphorus flame retardant and the carbon nanotubes play a synergistic flame-retardant role, so that the flame-retardant property of the rubber is remarkably improved.

The invention provides a non-aqueous electrolyte and a lithium ion battery. The non-aqueous electrolyte comprises a lithium salt, a non-aqueous organic solvent and an additive. The additive comprises a compound A as shown in a structural formula I; wherein R1 and R2 are respectively and independently selected from oxygen, sulfur or NR5, R3 and R4 are respectively and independently selected from NR6R7, R5 is C1-C5 alkyl silicon group, and R6 and R7 are respectively and independently selected from C1-C5 alkyl silicon group, C1-C5 alkyl group, substituted C1-C5 alkyl group, phenyl or substituted phenyl. The compound A comprises a cyclic (oxygen, sulfur and nitrogen) phosphamide structure and a trimethylsilyl structure, the trimethylsilyl structure can remove moisture in the electrolyte, and the cyclic (oxygen, sulfur and nitrogen) phosphamide structure is reduced on a negative electrode interface to form a polar solid electrolyte interface film of lithium salt containing oxygen or sulfur and phosphorus and nitrogen; the interfacial film has good lithium ion conductivity and toughness, the charge transfer resistance of the lithium ion battery is reduced, desolvation of lithium ions is promoted, and the high-rate cycle performance of the lithium ion battery is improved. The structural formula I of the # imgabs0 # is shown in the specification.

The invention belongs to the technical field of battery electrolyte, and particularly relates to flame-retardant cyclic phosphamide eutectic electrolyte as well as a preparation method and application thereof. According to the invention, through reasonable molecular design, the flame-retardant cyclic phosphamide eutectic electrolyte is obtained. Through the design of the annular structure, a film is formed on the positive and negative electrode interface of the electrode in the battery operation process, so that the stability of the battery is improved. Phosphamide groups are introduced into the cyclic structure, hydroxyl radicals generated in the battery operation process are captured through phosphorus-oxygen bonds, and the chain reaction of combustion is blocked. Meanwhile, different designs of amino groups on phosphamide can achieve a self-cleaning effect, hydrofluoric acid and water generated in a battery circulation process are removed, and the battery is protected from electrode structure collapse caused by the hydrofluoric acid and the water in an operation process. The safety performance of the lithium battery in the cycle process is obviously improved, and the development of the lithium battery with high safety and stable operation is effectively promoted. The preparation process is simple, safe to operate, high in purity and suitable for industrialization.

The invention belongs to the technical field of coupling reagents, and particularly discloses application of N-sulfonyl imidazolium salt as a coupling reagent, and the N-sulfonyl imidazolium salt as the coupling reagent is applied to synthesis of amide, dipeptide, polypeptide, carboxylic ester, carboxylic thioester, phosphamide and phosphate. According to the application of the N-sulfonyl imidazolium salt as the coupling reagent, compared with the prior art, the dosage of the coupling reagent is greatly reduced, the generation of byproducts is reduced, and the conversion rate of reactants is improved.

The invention relates to the technical field of biological medicines, and particularly discloses synthesis and application of oligonucleotide with a spacer group embedded between 5-terminal oxygen and thiophosphoric acid. The chemical modification strategy comprises the following steps: preparing a modified nucleotide phosphoramidite monomer in which a spacer group is embedded between O5'and thiophosphoric acid P (V); performing solid-phase synthesis on the modified nucleotide phosphoramidite monomer to construct a target oligonucleotide molecule; a spacer group is embedded between oxygen at the 5 '-terminal of the oligonucleotide and thiophosphoric acid P (V) to form a 5'-terminal thiophosphoric acid structure; as the terminal modified thiophosphoric acid belongs to a non-phosphatase substrate, the terminal modified thiophosphoric acid can resist exonuclease degradation and improve the biological activity of siRNA after being modified.

To provide a method for preparing oligonucleotides that can improve yields and purities of target phosphorodiamidate morpholino oligomers and reduce 4-nitrostyrene adduct impurities.SOLUTION: The process comprises: (a) converting a compound of Formula X-1 into a compound of Formula X-2: where R10 is a residue of an oligonucleotide (e.g., a phosphorodiamidate morpholino oligomer); R11 is an amine protecting group; wherein the compound of Formula X-1 is not bound to a solid support; and (b) optionally removing protecting groups in the compound of Formula X-2 to obtain the olignucleotide.SELECTED DRAWING: None

The invention discloses a method for detecting 5 '(E)-VPA phosphoramidite monomer related substances, and belongs to the technical field of liquid chromatography detection. Related substances comprise 5 '-(E)-VP-2'-OMe-A (Bz), 5 '(Z)-VPA, 5'-(E)-VP-2 '-OMe-A-CE-P and 5' (E)-VPA-OX, and chromatographic detection conditions comprise that the column temperature is 23-27 DEG C, a stationary phase of a chromatographic column is octadecyl bonded silica gel, a mobile phase A is an ammonium acetate solution, a mobile phase B is acetonitrile, gradient elution is performed, and the like. According to the method, four related substances in the 5 '(E)-VPA phosphoramidite monomer are effectively separated through specific liquid chromatography conditions, the system adaptability, specificity, linearity and range, detection limit, quantitation limit and accuracy verification of the method all meet acceptable standards of pharmacopoeia, and detection of multiple related substances can be completed within a short time; and a reliable means is provided for detecting and controlling the quality of the 5 '(E)-VPA phosphoramidite monomer.

An object is to provide an amidite monomer of diaminopurine and / or an amidite monomer of a thiouracil derivative suitable for use in synthesis of an acyclic single-stranded polynucleotide comprising diaminopurine and / or a thiouracil derivative by a phosphoramidite method. This object is achieved by an amidite monomer of diaminopurine and / or an amidite monomer of a thiouracil derivative protected with a specific protecting group removable by a base.

The present invention relates to small molecules having high affinity and specificity to prostrate-specific membrane antigen (PSMA) and methods of using them for therapeutic and diagnostic purposes.

The invention belongs to the technical field of medicinal chemistry, and relates to a novel small nucleic acid drug intermediate and a preparation method thereof, the intermediate is a 2 '-FANA-dU phosphoramidite monomer, the preparation method comprises the following steps: 1, reacting a compound a with a 33% hydrogen bromide-acetic acid solution in dichloromethane, and performing post-treatment to obtain a compound b; 2, reacting uracil and the like to generate a white solid, and reacting the white solid with the compound b to obtain a compound c; 3, reacting the compound c in methanol and ammonia water, crystallizing and drying to obtain a compound d; 4, the compound d reacts with 4, 4 '-dimethoxytriphenylchloromethane, and a compound e is obtained through treatment; 5, the compound e reacts with anhydrous diisopropyl imidazole and a 2-cyanoethyl-N, N, N ', N'-tetraisopropyl phosphoramidite reagent, and the 2 '-FANA-dU phosphoramidite monomer is obtained.The 2'-FANA-dU phosphoramidite monomer prepared through the method can modify siRNA, the biological activity of the siRNA can be reserved or even enhanced, and the biological stability of the siRNA can be remarkably improved.

The invention discloses synthesis of 5-nucleotide phosphorodithioamide and application of the 5-nucleotide phosphorodithioamide in oligonucleotide. The oligonucleotide modified by the phosphorodithioamide comprises nucleotide structural units shown in a formula I or a formula II,..., the formula I,..., the formula II. According to the invention, through specific limitation of the structure of a nucleotide dithiophosphoramide monomer, the prepared oligonucleotide comprises a 5-nucleotide dithiophosphoramide structural unit. Compared with a traditional oligonucleotide molecule, the oligonucleotide molecule modified by nucleotide dithiophosphoramide shows better enzymatic degradation resistance and pharmaceutical stability. In addition, the binding performance between the modified oligonucleotide molecules and environmental ions can be improved through nucleotide dithiophosphamide modification, and a novel chemical modification strategy is provided for research, development and application of oligonucleotide drugs.

The structure of the phosphoramidite cation is shown as follows: # imgabs0 #, wherein B is a basic group and is selected from one of A, U, C, G and T; r2 is alkyl, A2 is O or C, n is a natural number of 1-20, and X is selected from one of F, Cl, Br and I.

The invention discloses synthesis of 5 '-amino-3-nucleotide phosphamide and application of the 5'-amino-3-nucleotide phosphamide in oligonucleotide. The phosphamide modified oligonucleotide comprises a nucleotide structural unit shown as a formula I or a formula II,..., the formula I; ... formula II; through specific limitation of a nucleotide phosphamide monomer structure, the prepared oligonucleotide contains a phosphamide structural unit; compared with a traditional oligonucleotide molecule, the oligonucleotide molecule with the phosphamide modified nucleotide structure has more excellent effects on pharmaceutical parameters such as enzymatic degradation resistance, stability and the like, and in addition, phosphamide modification can improve the binding performance between the modified oligonucleotide molecule and environmental ions; a novel chemical modification strategy is provided for research, development and application of oligonucleotide drugs.

The invention provides a non-aqueous electrolyte and a lithium ion battery thereof. The non-aqueous electrolyte comprises an electrolyte salt, a non-aqueous organic solvent and an additive, wherein the additive comprises a bis (aziridinyl) phosphamide compound as shown in a structural formula I. Wherein R1 is selected from substituted or unsubstituted C1-C6 alkyl or substituted amino, the structural formula of the substituted amino is shown as a structural formula II or a structural formula III, R2, R3, R4, R5, R6, R7, R8, R9, R13, R14, R15 and R16 are respectively and independently selected from hydrogen and substituted or unsubstituted C1-C6 alkyl, and R11 and R12 are respectively and independently selected from substituted or unsubstituted C1-C6 alkyl. The mass ratio of the bis (aziridinyl) phosphamide compound is 0.01 to 1.00 percent. The non-aqueous electrolyte contains a specific flame retardant, can realize excellent flame retardant property only by low content, and has the flame retardant property and better high-temperature cycle and high-temperature storage performance when being used in the lithium ion battery. Structural formula I, structural formula II and structural formula III

The application discloses a five-membered ring containing alkynyl or triazole functional group P The chiral phosphine oxide compound is obtained through Domino Heck-Sonogashira cascade reaction by taking a prochiral tertiary phosphine oxide compound containing a double ethylene group and phenylacetylene as raw materials, transition metal palladium catalyst and chiral TADDOL phosphoramidite ligand under the protection of inert gas P The chiral phosphine oxide compound has a product yield of 96% and an enantioselectivity ee value of 99%, and a diastereoselectivity dr value of greater than 20:1. The application adopts an asymmetric desymmetrization strategy, uses a Heck reaction to start and a Sonogashira reaction to end a cascade reaction, simultaneously constructs P The chiral and quaternary carbon chiral center has mild reaction conditions, simple operation and good substrate universality, provides a compound skeleton with diversity, and is successfully applied to a palladium-catalyzed asymmetric allyl substitution reaction as a chiral ligand.

Provided is an oligonucleotide having excellent stability and capable of inducing ADAR editing activity in a cell. The oligonucleotide comprises a first oligonucleotide and a second oligonucleotide linked to the 5'side thereof, and induces site-specific editing against a target RNA. The first oligonucleotide is composed of a target-corresponding nucleotide residue, an oligonucleotide having 3 to 6 residues complementary to the target RNA on the 5'side thereof, and an oligonucleotide having 10 to 24 residues complementary to the target RNA on the 3 'side thereof. And at least one of a phosphorus-containing linking group connecting the nucleoside residues at the first position and the second position and a phosphorus-containing linking group connecting the nucleoside residues at the fourth position and the fifth position is an alkyl phosphonic acid residue, an alkyl phosphate residue or a substituted phosphamide residue. The second oligonucleotide has a nucleotide residue corresponding to the target RNA deleted at the 3'terminal, or has a nucleotide residue that does not form a complementary pair with the target RNA, the number of residues being 2 to 10, and the nucleotide residues other than the 3 'terminal being complementary to the target RNA.

This invention relates to the field of polyester materials technology, and discloses a flame-retardant biodegradable polyester material and its preparation method. The polyester material of this invention is composed of 65-80 parts by weight of aromatic polyester, 20-35 parts by weight of aliphatic polyester, and 5-25 parts by weight of polylactic acid-based flame retardant. The aromatic polyester is selected from polyethylene terephthalate (PET), and the aliphatic polyester includes biodegradable components such as polylactic acid (PLA). The PLA-based flame retardant of this invention improves the compatibility between aliphatic polyesters such as PLA and aromatic polyesters such as PET, resulting in better mechanical properties. Simultaneously, the main chain contains a large number of phosphoramide groups, forming a nitrogen-phosphorus flame-retardant system, thereby improving the flame-retardant performance of the polyester material.

A process for the hydrocyanation of an organic compound containing at least one olefinic group comprising reacting the organic compound with hydrogen cyanide in the presence of a catalyst complex comprising at least one transition metal and a phosphorus-containing ligand comprising a calixarene backbone and at least two aryl phosphite or aryl phosphoramidite groups chemically bonded to the backbone.

To provide methods for preparing phosphoramidites, which are useful for improving efficiency and / or lowering cost of oligonucleotide preparation.SOLUTION: A method for purifying a phosphoramidite comprises steps of: a) removing water from a purification medium; b) contacting the purification medium with a phosphoramidite; and c) optionally using the purification medium to purify a phosphoramidite.SELECTED DRAWING: Figure 1

The invention relates to the technical field of compound synthesis, in particular to a method for directly reducing carboxylic acid into aldehyde. The preparation method comprises the following steps: mixing triphenylphosphine, dichloromethane, carboxylic acid and N-chlorosuccinimide, and reacting to obtain a reactant; mixing with pinacol borane and 4-dimethyl pyridine, and continuously reacting to obtain a continuous reactant; and separating and purifying to obtain aldehyde. The synthesis of the substrate carboxylic acid provided by the invention and the rapid deoxidation of the carboxylic acid are carried out to obtain an aldehyde product, especially the following compounds 2aa, 2ab, 2ae, 2bc, 2be, 2bf, 2bg, 2bh, 2bi, 2bj, 2bk and 2bl have catalytic hydrolysis effects on hypophosphamide; the compound 2bl has a particularly excellent effect on hydrolysis of hypophosphamide.

This invention provides an oligonucleotide cleavage reagent (JS2 & S4 reagent) and its preparation method, as well as a method for cleaving oligonucleotides. The oligonucleotide cleavage reagent comprises NaOH, KOH, methanol, and a cleavage buffer. The oligonucleotide cleavage reagent JS2 & S4 and the cleavage method using it provided by this invention can efficiently cleave oligonucleotides, especially those synthesized using solid-phase phosphorous acid cleavage. This reduces chain breakage and side reactions caused by high-temperature cleavage, and also reduces equipment costs. While shortening the cleavage time, it can effectively reduce oligonucleotide quality problems caused by cleavage.

The utility model discloses cyclophosphamide preparation filling equipment, which belongs to the technical field of filling equipment and comprises a base, a filling component is mounted at the top end of a mounting rack, a fixed end of a stepping motor is mounted at the top end of the mounting rack, and a driving end of the stepping motor penetrates through the mounting rack and is connected with a rectangular mounting plate. The bottom end of the mounting plate is fixedly connected with a driving fixed end of a second electric push rod, the driving end of the second electric push rod is connected with a mounting box, a first screw rod for assisting adjustment is mounted on the inner side of the mounting box, and a servo motor for providing adjustment power for the first screw rod is mounted on the side face of the mounting box; the periphery of the first lead screw is in threaded connection with two symmetrical adjusting rods, the bottom ends of the adjusting rods penetrate through limiting grooves formed in the bottom end of the mounting box and are connected with clamping blocks, and the opposite faces of the two clamping blocks are each provided with an anti-skid pad in an adhesive mode. According to the cyclophosphamide preparation filling equipment, the sealing cover of the filling barrel can be automatically mounted, so that the filling operation is more time-saving and labor-saving.

The invention discloses an ultra-dispersed ceramic white switch panel master batch as well as a preparation method and application thereof. Relates to the field of polymer materials. The ultra-dispersed ceramic white switch panel master batch comprises the following components: carrier resin, a modified flame retardant, a dispersing agent and a pigment, molecules of the modified flame retardant contain a triazine ring, benzyl, a phosphamide group and chloroethyl, and the benzyl serves as a connecting unit and is connected with the triazine ring, the phosphamide group and the chloroethyl. According to the ultra-dispersed ceramic white switch panel master batch disclosed by the invention, multi-performance optimization is realized through a synergistic effect of specific components.

The disclosure relates to the production of highly pure N,N-diisopropylphosphoramidite compounds, such as 6-bromohexyl 2-cyanoethyl N,N-diisopropylphosphoramidite, and highly pure starting material used therein, such as 6-bromohexan-1-ol. The resulting N,N- diisopropylphosphoramidite compounds are useful, for example, for the improved preparation of expandable nucleotide triphosphates (XNTPs) for use in sequencing by expansion.

The invention discloses high-strength concrete and a curing method thereof, and belongs to the technical field of concrete. The high-strength concrete comprises the following components: 300-400 kg / m < 3 > of cement, 100-130 kg / m < 3 > of silica fume, 50-80 kg / m < 3 > of fly ash, 700-850 kg / m < 3 > of sand, 850-950 kg / m < 3 > of gravel, 5-9 kg / m < 3 > of a modified polycarboxylate superplasticizer and 140-170 kg / m < 3 > of water. The modified polycarboxylate superplasticizer is formed by copolymerizing a methacrylate functional monomer containing a phosphamide anchoring group, an imidazolium zwitterionic monomer containing a styryl group, an acrylic monomer, a monoethyl fumarate monomer and an allyl polyoxyethylene ether monomer. Through molecular design, a strong anchoring phosphamide group and a mud-resistant zwitterionic structural monomer are introduced into the polycarboxylate superplasticizer, so that the strength of concrete is improved, and the service life of the concrete is prolonged.

The invention relates to the technical field of biological medicine, and particularly discloses synthesis and application of oligonucleotide with threose nucleic acid 3-oxygen at the tail end indirectly connected with thiophosphoric acid. The chemical modification strategy comprises the following steps: O < 3->-oxygen of threose nucleic acid is connected with thiophosphoric acid through a spacer group, and O < 2->-hydroxyl is combined with a nucleotide monomer of phosphoramidite; carrying out solid-phase synthesis on the threose nucleic acid O2 '-phosphoramidite monomer to construct an oligonucleotide molecule; the oxygen of the threose nucleic acid at the terminal of the oligonucleotide is linked to the thiophosphoric acid through a spacer group, and since the type of phosphonic acid does not belong to a substrate of phosphatase, the modified oligonucleotide can resist exonuclease degradation and improve its in vivo biological activity.