87 results about "Leaving group" patented technology

The present invention provides a novel copolymer useful in drug delivery technology. The present invention relates to a drug complex obtained by binding a target-specific molecule to a copolymer X comprising structural units represented by formulae (A), (B) and (C). [In the formula, R1, R2 and R3 may be the same or different and each represents a hydrogen atom or a C1-3 alkyl group; r4 represents a C1-3 alkyl group; r5 represents a hydrogen atom, a C1-18 alkyl group, a 3-to 8-membered cycloalkyl group which may have a substituent, an adamantyl group, a C6-18 aryl group which may have a substituent, or a 5-to 10-membered heteroaryl group which may have a substituent; x1, X2, and X3 may be the same or different and each represents an oxygen atom, a sulfur atom, or N-R7; r6 represents a hydrogen atom, a leaving group or a linking group; r7 represents a hydrogen atom or a C1-3 alkyl group; m represents an integer of 1 to 100; and n represents an integer of 0-3. ] # imgabs0 #

A precursor compound and a radioligand for cancer diagnosis and treatment comprises a high-affinity ligand PL for a cancer- associated protein conjugated to a covalent warhead CW for strong or covalent binding to an amino acid sidechain of the cancer-associated protein and a chelator Ch for complexation of a radioisotope or a leaving group LR for substitution with a radioisotope, wherein the covalent warhead CW is configured for quasi-covalent ionic binding using a sulfonic acid group or for covalent binding using a sulfur fluoride exchange (SuFEx) group, a benzotriazole or N-methyl-N- arylmethanesulfonamide leaving group or a malolactone group for strain-release alkylation.

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.

A use of a compound of formula Y: (Y) to form a protected nucleophile, wherein a single substituent selected from R1-R4 is -CH2-LG or -CH2-OH, wherein LG is a leaving group; at least one substituent s

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 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.

Provided as a precursor of a radioactive halogen-labeled compound is a compound represented by the following general formula (I): wherein, R1 represents a leaving group capable of nucleophilic substitution by a halide ion, R2 represents a leaving group such that nucleophilic acyl substitution reaction is advanced by an amino group, and R3 represents a hydrogen atom or a halogen atom.

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.

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

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 relates to a method for purifying a compound of formula (IV-F), or a stereoisomer, racemic mixture, pharmaceutically acceptable salt, hydrate or solvate thereof, comprising a C1-4 alkyl sulfonate as a leaving group. The compounds of formula (IV-F) can be used as precursors to 18F-labeled agents for imaging and determining the amount of alpha-synuclein aggregates. The 18F-labelled agents may be used to diagnose a disease, disorder, or abnormality associated with alpha-synuclein aggregates (e.g., multi-system atrophy (MSA)), determine the susceptibility of such a disease, disorder, or abnormality, predict the prognosis of such a disease, disorder, or abnormality, monitor disease evolution in a patient suffering from such a disease, disorder, or abnormality, and, for example, to diagnose a disease, disorder, or abnormality associated with alpha-synuclein aggregates. The progression of such diseases, disorders or abnormalities is monitored, as well as the response of patients suffering from such diseases, disorders or abnormalities to their treatment is predicted. # imgabs0 #

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 present invention provides a method for preparing 6-isopropenyl-3-methyl-9-decenyl acetate (5), wherein Ac represents an acetyl group, and the method comprises the following steps: subjecting a 2-methyl-2,6-heptadiene compound (1) having a leaving group X at position 1 to a nucleophilic substitution reaction with a 3-methylpentyl nucleophile (2) having a protected hydroxyl group at position 5 to form a 6-isopropenyl-3-methyl-9-decene compound (3) having a protected hydroxyl group at position 1; subjecting the 6-isopropenyl-3-methyl-9-decene compound (3) having a protected hydroxyl group at position 1 to a deprotection reaction to form 6-isopropenyl-3-methyl-9-decenol (4); and acetylation of the 6-isopropenyl-3-methyl-9-decenol (4) to form 6-isopropenyl-3-methyl-9-decenyl acetate (5).

The invention discloses a fluorescent probe for detecting cysteine as well as a preparation method and a use method of the fluorescent probe. The invention designs a ratio type fluorescent probe BDP-SO-PEG7 (Benzo Bodipy) based on benzo Bodipy and PEG (Polyethylene Glycol) sulfoxide. A PEG sulfoxide part of the probe is a good leaving group and can be subjected to nucleophilic substitution reaction with sulfydryl of Cys to generate an intermediate product BDP-S-Cys, and then a final product BDP-N-Cys is generated through intramolecular rearrangement, so that the fluorescence change of the probe is caused. The ratio type fluorescent probe based on the benzo-Bodipy dye provided by the invention has good response performance to cysteine, and can realize sensitive, rapid and quantitative detection of trace cysteine in a sample. The probe has the advantages of simplicity and convenience in operation, low cost, sensitive response and the like, and is easy to popularize and apply.

The present invention aims to provide a method for producing a (2S,5R)-5-(protected oxyamino)-piperidine-2-carboxylic acid derivative at a low cost that can be performed under mild reaction conditions not requiring a facility at an extremely low temperature, is safer, can control the quality of the desired product with ease, and shows good workability in the site of production. A method for producing a compound represented by the formula (2):wherein PG1 is an amino-protecting group, PG2 is an amino-protecting group, PG3 is a hydroxyl-protecting group, LG is a leaving group, and R is a hydrocarbon group having 1-8 carbon atoms and optionally having substituent(s), including a step of reacting a compound represented by the formula (1):wherein each symbol is as defined above, with a hydroxylamine derivative represented by the formula PG2NHOPG3 wherein each symbol is as defined above, in the presence of a base in a solvent.

The invention provides a polymer contrast agent. The present invention pertains to a copolymer obtained by binding a chelating agent molecule to a copolymer X containing structural units represented by formulae (A), (B), and (C). [In the formula, R1, R2 and R3 may be the same or different and each represents a hydrogen atom or a C1-3 alkyl group; r4 represents a C1-3 alkyl group; r5 represents a hydrogen atom, a C1-18 alkyl group, a 3-to 8-membered cycloalkyl group which may have a substituent, an adamantyl group, a C6-18 aryl group which may have a substituent, or a 5-to 10-membered heteroaryl group which may have a substituent; x1, X2, and X3 may be the same or different and each represents an oxygen atom, a sulfur atom, or N-R7; r6 represents a hydrogen atom, a leaving group or a linking group; r7 represents a hydrogen atom or a C1-3 alkyl group; m represents an integer of 1 to 100; and n represents an integer of 0-3. ] # imgabs0 #

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.