62 results about "Leaving group" patented technology

The present invention relates to linker molecules of formula (1), X-Tb-Va—U—Y—Z (1) and a method for purifying peptides using said linker molecules. The linker molecule can be coupled to a purification resin via the moiety X and to a peptide via the moiety Y under the release of the leaving group Z. T is an optional spacer moiety and V is an optional electron withdrawing moiety. U is an aryl or 5- or 6-membered heteroaryl moiety bound to at least one electron withdrawing moiety V, W or E. The linker is stable under acidic conditions and releases the peptide upon addition of a reducing agent.

The invention discloses a continuous preparation method of a platinum bulk drug, which comprises the following steps: by taking chloroplatinite as a starting material, in a reaction environment of taking water as a solvent, replacing the starting material with iodized salt to obtain iodoplatinite, and then adding an amine ligand to quickly react to generate an intermediate-cis-diiodo-platinum-amine complex; introducing the solid-liquid mixed system containing the intermediate into a filtering and washing device, filtering and washing, directly discharging the solid into a reaction kettle, adding silver salt and water, reacting completely, and filtering; and concentrating the filtrate to obtain a crude product of the target product, and recrystallizing the crude product to obtain the platinum bulk drug. Or reacting the filtrate with a leaving group (or a salt formed by the leaving group) of the target compound, concentrating, filtering and washing to obtain a crude product of the target product, and recrystallizing the crude product to obtain the platinum bulk drug. The production efficiency and quality consistency of the product can be improved, the process amplification flow is simplified, the production cost and material consumption are reduced, green manufacturing is realized, and the method is an optimal choice for industrial production of platinum bulk drugs.

The invention discloses a synthesis method of 2, 4-dichloro-5-cyclopropylpyrimidine, which comprises the following steps: taking compounds 5-bromo-2, 4-dimethoxypyrimidine and cyclopropylboronic acid as raw materials, carrying out Suzuki-Miyaura coupling reaction to obtain an intermediate compound 5-cyclopropyl-2, 4-dimethoxypyrimidine, then taking phenylphosphonic dichloride as a chlorination reagent, and carrying out chlorination reaction to obtain the target compound 2, 4-dichloro-5-cyclopropylpyrimidine. The invention relates to 2, 4-dichloro-5-cyclopropyl pyrimidine. In the key steps, under the condition that phenylphosphonic dichloride is used as a chlorination reagent and a reaction solvent, through high-temperature reflux activation, methoxy as a leaving group is attacked by chlorine nucleophilic, methoxy (-OCH3) on a pyrimidine ring is substituted by a chlorine atom (-Cl), and the target product 2, 4-dichloro-5-cyclopropyl pyrimidine is generated. Finally, the target compound 2, 4-dichloro-5-cyclopropyl pyrimidine is obtained through short steps, simple and convenient operation, mild reaction conditions and ideal yield.

A copolymer includes a copolymer X and a chelating agent molecule bonded to the copolymer X. The copolymer X includes structural units of (A), (B), and (C),where R1, R2, and R3 are independently a hydrogen or a C1-3 alkyl, R4 is a C1-3 alkyl, R5 is a hydrogen, a C1-18 alkyl, a 3- to 8-membered cycloalkyl optionally having a substituent, an adamantyl, a C6-18 aryl optionally having a substituent, or a 5- to 10-membered heteroaryl group optionally having a substituent, X1, X2, and X3 are independently an oxygen, a sulfur, or N—R7, R6 is a hydrogen, a leaving group, or a linker, R7 is a hydrogen or a C1-3 alkyl group, m is an integer in the range of 1 to 100, and n is an integer in the range of 0 to 3.

A drug complex may include a target recognition molecule bonded to a copolymer X including structural units of (A), (B), and (C):R1, R2, and R3 being independently H or C1-3 alkyl, R4 being C1-3 alkyl, R5 being H, C1-18 alkyl, 3- to 8-membered cycloalkyl optionally being substituted, adamantyl, C6-18 aryl optionally being substituted, or 5- to 10-membered heteroaryl group optionally being substituted, X1, X2, and X3 being independent O, S, or N—R7, R6 being H, leaving group, or linker, R7 being H or C1-3 alkyl group, m being 1 to 100, and n being 0 to 3.

The Invention relates to a method Method for making a ruthenium catalyst comprising the steps of - Providing an aromatic dithiol substituted on adjacent aromatic carbon atoms with thiol groups, wherein in a first step an aromatic compound substituted with two leaving groups on adjacent aromatic carbon atoms are reacted with alkali trithiocarbonate to obtain an aromatic benzodithiole-thione, which in a subsequent step is reacted / hydrolysed with a base; - providing a zinc dithiolate compound by reacting the aromatic dithiol with a zinc carboxylate in an organic solvent; Reacting the zinc dithiolate compound with a ruthenium compound wherein X1 and X2 are, independently of each other, are anionic ligands and are the same or different; L and L2 are, independently of each other, neutral electron donor ligands and are the same or different; Ar is an aromatic group which may be substituted and that can be bridged with L, if L is an alkoxy group; - Obtaining a ruthenium catalyst of formula 4 or 4a, wherein R1 to R4 are, independently of each other, are selected from hydrogen, halogen, alkyl, aryl, or R.1 with R3, R3 with R4 or R2 with R4 are forming together an aliphatic or aromatic ring.

A method by which an intermediate product of an azole derivative can be produced at a lower cost than known production methods is provided. A method for producing a compound represented by General Formula (IV) includes converting a compound represented by General Formula (II) into the compound represented by General Formula (IV) using (a) dimethyl sulfide and / or dimethyl sulfoxide, and (b) a methyl-LG (an LG is a nucleophilically substitutable leaving group and is selected from the group consisting of a halogen group, an alkoxysulfonyloxy group, an aryloxysulfonyloxy group, an alkylsulfonyloxy group, a haloalkylsulfonyloxy group, and an arylsulfonyloxy group) in the presence of an inorganic base.

A method comprising co-administering to a subject having cancer, suspected of having cancer, or at risk of developing cancer:a therapeutically effective amount of at least one compound (a) selected from (a)(i) a nitroalkene fatty acid, (a)(ii) an unsaturated fatty acid having an electron withdrawing group, a leaving group, and a carbon-carbon double bond disposed between the electron withdrawing group and the leaving group, (a)(iii) a thiolated nitro fatty acid, or (a)(iv) a dicarboxylic acid compound containing an electron withdrawing group; anda therapeutically effective amount of at least one anti-neoplastic agent (b),wherein the cancer is a cancer with hereditary etiology of defects in DNA repair genes, a cancer with a high rate of spontaneous genomic instability, a cancer that responds well to DNA damaging agent(s), or a cancer that responds well to a combination of DNA damaging agent(s) with immunotherapy.

Exemplary embodiments of the present technological advancement include pyridine-2,6-bis(phenylenephenolate) complexes that are useful as catalyst components for olefin polymerization and have enhanced solubility in non-aromatic hydrocarbons (e.g., isohexane). The improved solubility of these complexes was accomplished by the modification of the leaving group which generally leads to improved solubility, without adversely affecting the performance of the complex when used as a catalyst for olefin polymerizations.

The application discloses tetraacetyldicyclopropylhexaazaisowurtzitane and a preparation method thereof, and a synthesis method of HNIW, and belongs to the technical field of chemical synthesis. The tetraacetyldicyclopropylhexaazaisowurtzitane is a new hexaazaisowurtzitane derivative, the preparation method has short reaction steps, simple operation, and raw materials are easy to obtain, and has industrial application potential. The tetraacetyldicyclopropylhexaazaisowurtzitane can be used for synthesizing hexanitrohexaazaisowurtzitane (HNIW) through nitration, the synthesis process is simplified, and the production cost is reduced; the leaving group cyclopropyl has a small proportion in the cyclopropylamine raw material, has good atom economy, has high raw material utilization, reduces waste emission, and meets the environmental protection concept of green economy.

Disclosed is a supported catalyst system comprising a substituted 2-hydroxythiophene compound and a support material; and a process for preparing the supported catalyst system; also disclosed is a gas phase or slurry phase polymerization process employing the supported catalyst system; and a polyolefin prepared by the gas phase or slurry phase polymerization process. The substituted 2-hydroxythiophene compound and a pre-catalyst comprising the substituted 2-hydroxythiophene compound, a metal atom, and a leaving group are also disclosed. Methods of preparing the pre-catalyst and the substituted 2-hydroxythiophene compound are also disclosed.

The invention relates to a silicon-containing resist film forming composition and a pattern forming method. The present invention is a silicon-containing composition for forming a resist film, which forms an ultra-fine resist pattern having excellent LWR and CDU, which forms a resist film having high etching selectivity with an organic material, and which does not cause defects due to residues remaining after the completion of patterning, and a pattern forming method. A silicon-containing composition for forming a resist film, which contains a polysiloxane that contains at least one of a repeating unit represented by formula (A-1), a repeating unit represented by formula (A-2), and a partial structure represented by formula (A-3). (In the formula, R1 is a C1-30 monovalent organic group which may have a substituent and acts as a leaving group by heat, an acid or a base, a halogen atom, a hydroxyl group, a sulfo group, a nitro group or a carboxyl group, and R2 and R3 each independently represent a C1-30 monovalent organic group which may have a substituent.

The present invention discloses a fluorescent probe for detecting cysteine, and its preparation and use methods. The present invention designs a ratiometric fluorescent probe BDP-4SPy based on benzo-BodiPy and 4-mercaptopyridine. The thiopyridine portion of the probe is a good leaving group. It undergoes nucleophilic substitution with the thiol group of Cys to generate BDP-S-Cys, which is then subjected to intramolecular rearrangement to generate BDP-N-Cys, thereby causing a change in the probe fluorescence. The ratiometric fluorescent probe of the benzo-BodiPy dye provided by the present invention has good response performance to cysteine, can achieve sensitive, rapid, and quantitative detection of trace cysteine ​​in a sample, and has the advantages of simple operation, low cost, sensitive response, and easy promotion and application.

The present invention provides a compound or a salt thereof which is used in the preparation of a linker that can easily obtain an antibody drug complex having a uniform structure and stability in blood. A compound represented by general formula [ML-I] or a salt thereof is disclosed as the compound or the salt thereof. # imgabs0 # [wherein X is a leaving group; r1 and R2 are each independently hydrogen, C1-6 alkyl which may be substituted by one or more substituents, or C1-6 alkylene-R11 which may be substituted by one or more substituents (however, R1 and R2 are not hydrogen at the same time); alternatively, R1 and R2, together with adjacent nitrogen atoms, form a 7-membered ring which further contains a nitrogen atom as a ring constituent atom, and the ring further has, as a substituent,-C (= O)-C1-6 alkylene-R11 which may be substituted with one or more substituents; r11 is COOH, SO3H or PO3H2, or ester group thereof]

Disclosed is a supported catalyst system comprising a substituted 2-hydroxythiophene compound and a support material; and a process for preparing the supported catalyst system; also disclosed is a gas phase or slurry phase polymerization process employing the supported catalyst system; and a polyolefin prepared by the gas phase or slurry phase polymerization process. The substituted 2-hydroxythiophene compound and a pre-catalyst comprising the substituted 2-hydroxythiophene compound, a metal atom, and a leaving group are also disclosed. Methods of preparing the pre-catalyst and the substituted 2-hydroxythiophene compound are also disclosed.

An acetal-type releasable polyoxyethylene derivative is expressed by the Formula (1), (2), (3) or (4) as defined herein, and cleaved under a physiological condition, and in the formulas (1), (2), (3) and (4), B1 represents a hydrogen atom or —C(R1)(R2)OC(O)E1, E1 represents a leaving group, P1 represents a polyoxyethylene derivative having a dehydroxylated group, w represents an integer of 1 to 8, R1, R2, R3, R4, R5 and R11 each independently represent a hydrocarbon group having 1 to 10 carbon atoms or a hydrogen atom, R6, R7, R8, R9 and R10 each independently represent an electron-withdrawing substituent, an electron-donating substituent, or a hydrogen atom, and m represents 0 or 1.

The present invention provides: a method for producing a sulfonic acid ester, with which it is possible to produce a sulfonic acid ester with a high yield; a method for producing a fluorosulfonyl group-containing compound; a method for producing a polymer; a method for producing a liquid composition; a method for producing a membrane; a method for producing a membrane electrode assembly; and a compound. The membrane and the membrane electrode assembly can be used, for example, in fuel cells and PEM water electrolysis applications.　With the method for producing a sulfonic acid ester according to the present invention, a compound represented by formula (3) is obtained by reacting a compound represented by formula (1) with a compound represented by formula (2). In formulae (1) to (3), R is an n-valent aliphatic hydrocarbon group which may have an aromatic hydrocarbon group as a substituent, and the aliphatic hydrocarbon group may have an etheric oxygen atom or -CO- between carbon atom-carbon atom bonds. Z+ is a monovalent cation, n is a number of 1 to 4, X is a hydrogen atom or a halogen atom, and Y is a monovalent leaving group. (1): R-(SO2O-Z+)n, (2): CFX=CF-CF2-Y, (3): R-(SO2O-CFX-CF=CF2)n

This invention discloses a highly efficient oxygen removal reagent and its application in the deoxygenation reconstruction of carbon resource molecular skeletons, comprising a pivot reagent, a phosphine reagent, an azo reagent, a reducing agent, an acid reagent, a base reagent, a photosensitizer, and an organic solvent; wherein, X in the pivot reagent includes a hydrazine group or a sulfone group; PG is a protecting group; LG is a leaving group; by using natural oxygen-containing functional groups such as alcohols, aldehydes, and ketones as direct coupling precursors, an integrated in-situ activation-deoxygenation coupling process is achieved, significantly reducing reaction steps.

The application belongs to the technical field of organic synthesis and particularly relates to a preparation method of riboprine. The method comprises the following steps: starting from a key intermediate (1S, 5R)-1-(3-fluorophenyl)-3-oxabicyclo[3.1.0]hexan-2-one, hydrolysis is performed to form an open ring compound, then a protecting group of a hydroxyl group is introduced under alkaline conditions; then, reduction is performed on a carboxyl group to form a hydroxyl compound, an intermediate compound is generated by introducing a leaving group and then reacting with 2, 4-dimethyl-5-hydroxypyrimidine, the protecting group is removed to expose the hydroxyl group, oxidation is performed to form a carboxyl compound, and finally, acid-amine condensation reaction is performed on 2-amino-5-fluoropyridine to generate riboprine. The preparation method provided by the present application is simple in operation, high in yield and suitable for industrial production of riboprine.

The present invention relates to the technical field of biomedicine, and in particular to a preparation method for 18F-DOPA and an F-18-labeled precursor thereof. The structural formula of an F-18-labeled phenolic precursor compound is as shown in formula I, wherein R1 and R2 are hydroxyl protecting groups; R3 is a leaving group; R4 and R5 are each independently hydrogen or an amino protecting group; and R6 is a carboxyl protecting group. The present invention provides a simple and efficient preparation method for 18F-DOPA, specifically by constructing a key phenolic precursor compound and by means of a simple and efficient photocatalytic aromatic hydrocarbon deoxyfluorination reaction to implement the preparation of 18F-DOPA. The method has fewer steps, high yield, simple and convenient operation, good reproducibility, and good automated production potential. The radiotracer 18F-DOPA synthesized by means of the method has high specific activity and high chemical purity and radiochemical purity, and has significant value for the clinical promotion of 18F-DOPA.

The invention discloses a preparation method of flunarizine hydrochloride, which comprises the following steps: adding bis-(4-fluorophenyl) methyl alcohol into an organic solvent, adding an alkali solution, dropwise adding a TsCl solution, carrying out post-treatment to obtain a p-toluenesulfonic acid bis-(4-fluorophenyl) methyl ester solid, reacting with cinnamyl piperazine to obtain flunarizine free alkali, and carrying out post-treatment on the flunarizine free alkali to obtain the flunarizine hydrochloride. And finally, acidizing and recrystallizing to obtain flunarizine hydrochloride. According to the method, more efficient leaving groups are adopted, the reaction time is short, the operation is simple, crystallized solid p-toluenesulfonic acid bis-(4-fluorophenyl) methyl ester is obtained through post-treatment, and industrial production is facilitated.

Methods, compounds and combinations useful for treating or delaying progression of cancer or reducing ascites formation or volume in an individual comprising administering to the individual an effective amount of a PARP inhibitor and a compound of Formula I: wherein R is H, an in vivo cleavable linker or group, or a leaving group in aqueous solution and R1 and R2 are independently, H, alkyl, an aryl, a substituted alkyl, a substituted phenyl, a substituted aryl, or a combination thereof.

The invention discloses a hexaazaisowurtzitane derivative, a preparation method of the hexaazaisowurtzitane derivative and a synthesis method of HNIW, and belongs to the technical field of chemical synthesis. The preparation method of the hexaazaisowurtzitane derivative has the advantages of short reaction steps, simple operation, easily available raw materials and industrial application potential. The hexaazaisowurtzitane derivative disclosed by the invention can be used for synthesizing hexanitrohexaazaisowurtzitane (HNIW) in one step through nitration, so that the synthesis process is simplified, and the production cost is reduced; the specific gravity of the leaving group cyclopropyl in the cyclopropylamine raw material is small, the atom economy is good, the utilization rate of the raw material is high, waste discharge is reduced, and the method conforms to the environmental protection concept of green economy.

The present invention provides dual-functional tetrazine compounds for labeling with either metals including radiometals or with halogens including radiohalogens suitable for therapeutic or diagnostic purposes. Alternatively, the tetrazines can be used as precursors for labeling with a radiohalogen when the compound comprises a leaving group. The tetrazines are specifically engineered to facilitate efficient and stable incorporation of various radionuclides. By integrating a chelator group for radiometals and a leaving group for radiohalogens, these tetrazines offer a flexible and interchangeable structure that facilitates the development of radiopharmaceuticals. The tetrazines are for use in pretargeting therapy, diagnostics, imaging and theranostics. Use of the precursors for labeling with radiohalogen and use of the tetrazines as reagent in tetrazine ligation is moreover disclosed.

The invention discloses a method for synthesizing an alkylindole derivative based on a polarity reversal strategy, and belongs to the technical field of organic synthesis. Based on a polarity reversal strategy, polarity reversal of an indole substrate is achieved by connecting a leaving group to the indole substrate, a Grignard reagent is adopted as a nucleophilic reagent for reaction, region selectivity of the reaction is regulated and controlled under the action of a copper catalyst, and efficient synthesis of a series of C3-alkylindole and N-alkylindole is achieved; the reaction system provided by the invention is efficient and simple, is convenient to operate, has wide substrate applicability, can be used for synthesizing alkylindole derivatives which are difficult to synthesize by adopting other methods, provides an efficient synthesis method for the compounds, and has a better application prospect.

The invention discloses a preparation method of a C-H nitrated compound of unactivated aromatic hydrocarbon, which comprises the following steps: at room temperature, adding a compound 1, a nitro source, an oxidant, a catalyst and an organic solvent into a reaction tube, placing the reaction tube in an oil bath environment, and carrying out heating and stirring reaction; and after the reaction is finished, carrying out reduced pressure distillation on the reaction system, and purifying through a silica gel column to obtain a nitro compound product, namely a compound 2, with a reaction formula as shown in the specification. Wherein the number of substituent groups R on a benzene ring is 1-2, and each substituent group is independently selected from halogen, nitro, cyano, C1-C4 alkoxy, ester group, amino, pyrimidyl or pyridyl. According to the method disclosed by the invention, other leaving groups, reaction intermediates and guiding groups are not introduced in the reaction process, and the used nitro source does not cause adverse side reactions to the reaction and does not limit the application range of a substrate.

The present invention provides a crosslinking agent which can improve crosslinked fluoroelastomer high-temperature vapor resistance and a crosslinked fluoroelastomer having improved high-temperature vapor resistance. The present invention provides a compound having a structure represented by the following formula (1) (in the formula, R1 to R6 are each a hydrogen atom, a substituent, or a leaving group, and two or more of R1 to R6 are leaving groups; Ra to Rc are each a hydrogen atom or a substituent; and n is an integer from 2 to 5).

This invention provides a method for synthesizing liquid crystal compounds. This method uses dihaloalkanes and difluoromethane with leaving groups as raw materials to synthesize liquid crystal compounds while ensuring high yield and significantly reducing production costs.

The invention belongs to the technical field of organic synthesis, and particularly relates to a preparation method of lybolisan. The method comprises the following steps: hydrolyzing a key intermediate (1S, 5R)-1-(3-fluorophenyl)-3-oxabicyclo [3.1. 0] hexane-2 ketone to form a ring-opening compound, and introducing a hydroxyl protecting group under an alkaline condition; the method comprises the following steps: firstly, preparing a carboxyl group, then reducing the carboxyl group to form a hydroxyl compound, introducing a leaving group, then reacting with 2, 4-dimethyl-5-hydroxypyrimidine to generate an intermediate compound, then removing a protecting group to expose the hydroxyl group, carrying out oxidation reaction to form a carboxyl compound, and finally, carrying out acid amine condensation reaction with 2-amino-5-fluoropyridine to generate the lybula. Reagents used in the preparation method are cheap and easy to obtain, operation is easy, the yield is high, and the preparation method is suitable for industrial production of the libolifera.

Disclosed is a supported catalyst system comprising a substituted 2-hydroxythiophene compound and a support material; and a process for preparing the supported catalyst system; also disclosed is a gas phase or slurry phase polymerization process employing the supported catalyst system; and a polyolefin prepared by the gas phase or slurry phase polymerization process. The substituted 2-hydroxythiophene compound and a pre-catalyst comprising the substituted 2-hydroxythiophene compound, a metal atom, and a leaving group are also disclosed. Methods of preparing the pre-catalyst and the substituted 2-hydroxythiophene compound are also disclosed.