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3921 results about "Protecting group" patented technology

A protecting group or protective group is introduced into a molecule by chemical modification of a functional group to obtain chemoselectivity in a subsequent chemical reaction. It plays an important role in multistep organic synthesis.

Polymer sacrificial light absorbing structure and method

Method and structure for optimizing dual damascene patterning with polymeric dielectric materials are disclosed. Certain embodiments of the invention comprise polymeric sacrificial light absorbing materials (“polymer SLAM”) functionalized to have a controllable solubility switch wherein such polymeric materials have substantially the same etch rate as conventionally utilized polymeric dielectric materials, and subsequent to chemical modification of solubility-modifying protecting groups comprising the SLAM materials by thermal treatment or in-situ generation of an acid, such SLAM materials become soluble in weak bases, such as those conventionally utilized to remove materials in lithography treatments.
Owner:INTEL CORP

Pyrrolobenzodiazepines

A compound of formula (I) and salts and solvates thereof, wherein: R10 is a nitrogen protecting group and R11 is either OH or O—R12, wherein R12 is an oxygen protecting group, or R10 and R11 together form a double bond between N10 and C11; and R10′ and R11′ are selected from the same options as R10 and R11 respectively.
Owner:MEDIMMUNE LTD

PNA monomer and precursor

This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: whereinR1, R2, R3, R4, R5 is independently H, halogen, C1–C4 alkyl, nitro, nitrile, C1–C4 alkoxy, halogenated C1–C4 alkyl, or halogenated C1–C4 alkoxy, wherein at least one of R1, R3, and R5 is nitro;R6 is H or protected or unprotected side chain of natural or unnatural α-amino acid; andB is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases.
Owner:PANAGENE INC

Thiocarbon-protecting groups for RNA synthesis

Aspects of the invention include 2′ protected nucleoside monomers that are protected at the 2′ site with thiocarbon protecting groups. Thiocarbon protecting groups of interest include thiocarbonate, thionocarbonate, dithiocarbonate groups, as well as thionocarbamate protecting groups. Aspects of the invention further include nucleic acids that include the protecting groups of the invention, as well as methods of synthesizing nucleic acids using the protecting groups of the invention.
Owner:AGILENT TECH INC +1

Phosphinoamidite carboxylates and analogs thereof in the synthesis of oligonucleotides having reduced internucleotide charge

Nucleoside phosphinoamidite carboxylates and analogs are provided that have the structure of formula (III)wherein A is hydrogen, hydroxyl, lower alkoxy, lower alkoxy-substituted lower alkoxy, halogen, SH, NH2, azide or DL wherein D is O, S or NH and L is a heteroatom-protecting group, unsubstituted hydrocarbyl, substituted hydrocarbyl, heteroatom-containing hydrocarbyl, or substituted heteroatom-containing hydrocarbyl; B is a nucleobase; and one of R11 and R12 is a blocking group and the other is (IV) or (VI)in which W, X, Y, Z, R1 and n are as defined herein.
Owner:AGILENT TECH INC

2′-silyl containing thiocarbonate protecting groups for RNA synthesis

Nucleoside monomers, nucleic acids, e.g., oligonucleotides and polynucleotides, methods of making each, methods of deprotecting each, and the like are disclosed herein. Aspects of the invention include 2′ silyl containing thiocarbonate protecting groups. Corresponding compositions and methods are provided.
Owner:UNIV OF COLORADO THE REGENTS OF +1

Library of compounds comprising pyrrolobenzodiazepine moieties

A compound of formula (IV): O is a solid support; L is a linking group or a single bond; X′ is selected from CO, NH, S, or O; A is O, S, NH, or a single bond; R2 and R3 are independently selected from: H, R, OH, OR, ═O, ═CH—R, ═CH2, CH2—CO2R, CH2—CO2H, CH2—SO2R, O—SO2R, CO2R, COR, CN and there is optionally a double bond between C1 and C2 or C2 and C3; R6, R7, and R9 are independently selected from H, R, OH, OR, halo, nitro, amino, Me3Sn; R11 is either H or R; Q is S, O or NH; R10 is a nitrogen protecting group; and Y is a divalent group such that HY═R, and other related compounds and collections of compounds.
Owner:MEDIMMUNE LTD

Method for synthesizing tyrosine kinase inhibitor PCI-32765

The invention discloses a method for synthesizing tyrosine kinase inhibitor PCI-32765. The method comprises the following steps of: 1) carrying out a coupled reaction between a compound 10 and a compound 15 to obtain a compound 6; 2) reacting the compound 6 with a compound 16 to obtain a compound 11 in the presence of a more ideal catalyst; 3) protecting the compound 11 to obtain a compound 12; 4) carrying out selective de-protection on the compound 12 to obtain a compound 13; 5) attacking the compound 13 which has only one position which can be attacked by a compound 17 to obtain a very pure compound 14; and 6) removing protecting groups, thus obtaining the PCI-32765. By the method, tyrosine kinase which serves as a main receptor signal of B cells can be inhibited, and the tyrosine kinase inhibitor PCI-32765 is not only capable of inhabiting the generation of hemocyte with little toxicity and side effects, but also is moderate in reaction conditions, simple to operate, convenient to purify, low in cost, environment-friendly, and suitable for large scale production.
Owner:SUZHOU DEVI PHARMA TECH CO LTD

Protecting groups for RNA synthesis

Aspects of the invention include 2′ protected nucleoside monomers that are protected at the 2′ site with orthoester-type protecting groups. The 2′ protected monomers also include a second, aryl carbonate-type, protecting group. Aspects of the invention further include nucleic acids that include the protecting groups of the invention, as well as methods of synthesizing nucleic acids using the protecting groups of the invention.
Owner:UNIV OF COLORADO THE REGENTS OF +1

Preparation method of ticagrelor

The invention provides a preparation method of ticagrelor, belonging to the technical field of medicine manufacturing. According to the method, a compound VII is taken as a raw material, and the method comprises the steps of: carrying out a nucleophilic substitution reaction on the raw material to obtain a compound VI; hydrogenating the VI, removing carbamazepine (Cbz) protection to obtain a compound V; carrying out a reaction on the V and 4, 6-dichloro-2-(allyl sulfide)-5-amio-pyrimidine to obtain a compound IV; carrying out a reaction on the IV and nitrite of alkali metal to obtain a compound III; carrying out a reaction on the III and (1R, 2S)-2-(3, 4-difluoro phenyl) cyclopropylamine to obtain a compound II; and finally, removing protecting group of the II to obtain a compound I.
Owner:SHANGHAI HAOYUAN CHEMEXPRESS

Ester compounds, polymers, resist composition and patterning process

A novel ester compound having an alkylcycloalkyl or alkylcycloalkenyl group as the protective group is provided as well as a polymer comprising units of the ester compound. The polymer is used as a base resin to formulate a resist composition having a higher sensitivity, resolution and etching resistance than conventional resist compositions.
Owner:SHIN ETSU CHEM IND CO LTD

Protected nucleotide analogs

Disclosed herein are nucleotide analogs with one or more protecting groups, methods of synthesizing nucleotide analogs with one or more protecting groups and methods of treating diseases and / or conditions such as viral infections, cancer, and / or parasitic diseases with the nucleotide analogs with one or more protecting groups.
Owner:ALIOS BIOPHARMA INC

Bicyclonucleoside analogues

Bicyclonucleoside analogues which exhibit anti-AIDS activity and intermediates to produce oligonucleotide analogues which have anti-sense or anti-gene activity as well as in vivo stability. Compounds of the following formula (1) or their pharmaceutically acceptable salts.wherein R1 represents a hydrogen atom or a protecting group for a hydroxy group, R2 represents an azido group or an optionally protected amino group or the like, B represents a purin-9-yl or a 2-oxo-1,2-dihydropyrimidin-1-yl group, which are optionally substituted with substituents selected from the group consisting of a halogen atom, an alkyl group having 1–6 carbon atoms, a hydroxy group, a mercapto group and an amino group.
Owner:IMANISHI TAKESHI

Process for the preparation of pyrimidine derivatives

ActiveUS20050124639A1Easier and economical productionSimple reaction conditionsBiocideOrganic active ingredientsOxygenAldehyde
An improved process for the preparation of pyrimidine derivatives is provided comprising reacting a Wittig reagent of the general formula wherein R is an alkyl of from 1 to 10 carbon atoms, aryl or arylalkyl, R1 is a substituted or unsubstituted hydrocarbon group, R2 and R3 are the same or different and are hydrogen or a substituted or unsubstituted hydrocarbon group; Z is sulfur, oxygen, sulfonyl, or imino which may be substituted by formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, amino substituted by sulfonyl or alkylsulfonyl, and sulfonyl substituted by alkyl, amino or alkylamino and X is a halogen; with an aldehyde of the general formula wherein R4 is hydrogen, a lower alkyl or a cation capable of forming a non-toxic pharmaceutically acceptable salt and each R5 are the same or different and are hydrogen or a hydrolyzable protecting group, or each R5, together with the oxygen atom to which each is bonded, form a hydrolyzable cyclic protecting group, or each R5 is bonded to the same substituent which is bonded to each oxygen atom to form a hydrolyzable protecting group; in the presence of a base.
Owner:GLENMARK LIFE SCI LTD

Conformationally constrained backbone cyclized peptide analogs

InactiveUS7084244B2Peptide-nucleic acidsKallidins/bradykininsSomatostatin analogSide chain
Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are Nα(ω-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these Nα(ω-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is specifically exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.
Owner:DEVELOGEN ISRAEL

Synthesis of polynucleotides using combined oxidation/deprotection chemistry

A method of synthesizing a polynucleotide which can, for example, be used during fabrication of an array. A second nucleoside is coupled to a first nucleoside through a phosphite linkage, with the second nucleoside having a hydroxyl protecting group that is a non-carbonate protecting group. The product of the foregoing step is exposed to a composition which both oxidizes the formed phosphite to a phosphate and deprotects the protected hydroxyl of the coupled nucleoside. The method has particular application to fabricating an addressable array of polynucleotides on a substrate which carries substrate bound moieties each with a hydroxyl group.
Owner:UNIV OF COLORADO THE REGENTS OF +1

Methods of synthesizing oligonucleotides using carbonate protecting groups and alpha-effect nucleophile deprotection

The invention provides methods for synthesizing oligonucleotides using nucleoside monomers having carbonate protected hydroxyl groups that are deprotected with α-effect nucleophiles. The α-effect nucleophile irreversibly cleave the carbonate protecting groups while simultaneously oxidizing the internucleotide phosphite triester linkage to a phosphodiester linkage. The procedure may be carried out in aqueous solution at neutral to mildly basic pH. The method eliminates the need for separate deprotection and oxidation steps, and, since the use of acid to remove protecting groups is unnecessary, acid-induced depurination is avoided. Fluorescent or other readily detectable carbonate protecting groups can be used, enabling monitoring of individual reaction steps during oligonucleotide synthesis. The invention is particularly useful in the highly parallel, microscale synthesis of oligonucleotides.
Owner:AGILENT TECH INC +1

Thioester derivatives of thiazolyl acetic acid and their use in the preparation of cephalosporin compounds

The present invention provides novel thioester derivatives of thiazolyl acetic acid of the general formula (I),wherein, R1 represents H, trityl, CH3, or CRaRbCOOR3, in which Ra and Rb, independently of one another, represents hydrogen or methyl and R3 represents H or C1-C7 alkyl; and R2 represents C1-C4 alkyl or phenyl. The invention also provides a method for preparation of the thioester derivatives and reaction of the thioester derivatives with cephem carboxylic acids to produce cephalosporin antibiotic compounds having general formula (II),wherein, R1 represents H, trityl, CH3, or CRaRbCOOR3, in which Ra and Rb, independently of one another, represents hydrogen or methyl and R3 represents H or C1-C7 alkyl; R4 is CH3, -CH=CH2, CH2OCH3, CH2OCOCH3,and R5 is H or a salt or a carboxylic protecting group, comprising,acylating a compound of formula (III),wherein, R4 and R5 are defined as above, and R6 is H or trimethylsilyl;with a compound of formula (I).
Owner:ORCHID CHEM & PHARM LTD

Phosphorus protecting groups

Compounds having a phosphorus group structure of:wherein:R is alkyl, modified lower alkyl; andRi and Ri are each independently H, alkyl, modified alkyl, or aryl; are provided. Also provided are polynucleotide compositions that include these compounds and methods of using the compounds in synthesis of the same.
Owner:UNIV OF COLORADO THE REGENTS OF +1

Orally administered peptides to ameliorate atherosclerosis

InactiveUS7144862B2Readily taken up and deliveredMany symptomAntibacterial agentsBiocideAmphipathic helixMedicine
This invention provides novel peptides that ameliorate one or more symptoms of atherosclerosis. In certain embodiments, the peptide comprises an amino acid sequence that ranges in length from about 10 up to about 30 amino acids, that comprises at least one class A amphipathic helix, that bears at least one protecting group, that protects a phospholipid against oxidation by an oxidizing agent; and that is not the D-18A peptide. The peptides are highly stable and readily administered via an oral route.
Owner:UAB RES FOUND +1
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