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7388094 |
Processing for producing 2′-deoxy-2′-fluorouridine
1-β-D-Arabinofuranosyluracil in 3′,5′-hydroxyl-protected form is reacted with a trifluoromethanesulfonylating agent in the presence of an organic base to convert it into a 2′-triflate form,...
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7365188 |
Process for producing N4-Acyl-5′-deoxy-5-fluorocytidine
The present invention provides a process for producing a N 4 -acyl-5′-deoxy-5-fluorocytidine compound of the formula:
where R 2 is alkyl, cycloalkyl, aralkyl, aryl, or alkoxy.
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7345164 |
Production method of 5′-acyloxynucleoside compound
A production method for conveniently producing a 5′-acyloxynucleoside compound shown by the formula [A] in a good yield while suppressing formation of by-products, including subjecting a...
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7342003 |
Synthesis of 2-aralkyloxyadenosines, 2-alkoxyadenosines, and their analogs
Provided is a method for the synthesis of an aralkyloxyadenosine or an alkoxyadenosine. The method includes protecting the hydroxyl sugar groups with a protecting group to produce a protected...
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7339054 |
Process for preparing branched ribonucleosides from 1,2-anhydroribofuranose intermediates
A process is provided for the preparation of branched-chain ribonucleosides of formula (I):
from the 1,2-anhydroderivatives of formula (II).
wherein PG is a hydroxyl protecting group, B is...
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7297787 |
Process for preparing N6 substituted aminopurine ribofuranose nucleosides
An improved process for preparing N6 -substituted aminopurine ribofuranose nucleosides. Compounds of this type are known to be usefull in the prepartation of compounds having activitity at...
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7291726 |
Process for the preparation of 2′-halo-β-L-arabinofuranosyl nucleosides
The present invention is directed to the process for the preparation of 2′-deoxy-2′-halo-β-L-arabinofuranosyl nucleosides, and in particular, 2′-deoxy-2′-fluoro-β-L-arabinofuranosyl...
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7101994 |
Process for preparing substituted benzimidazole compounds
The invention relates to new methods of preparing substituted benzimidazole compounds, such as 2-bromo-5,6-dichlorobenzimidazole, which are useful in the preparation of compounds having antiviral...
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7038039 |
Process for selectively producing 1-phosphorylated sugar derivative anomer and process for producing nucleoside
A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the...
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7019128 |
Propargylethoxyamino nucleotides
Propargylethoxyamino nucleosides are disclosed having the structure
wherein R 1 and R 2 are —H, lower alkyl, or label; B is a 7-deazapurine, purine, or pyrimidine nucleoside base; W 1 is...
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7002006 |
Protection of nucleosides
A process of manufacturing protected nucleosides comprises reacting a nucleoside with a protecting reagent in the presence of a regioselective activator to produce a regioselectively protected...
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6972330 |
Chemical synthesis of methoxy nucleosides
Process for chemical synthesis of methoxy nucleosides.
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6914138 |
Urea nucleosides as therapeutic and diagnostic agents
Modified nucleosides and methods of making and using the nucleosides are disclosed. The compounds can be prepared by reacting nucleoside starting materials that contain a suitable leaving group at...
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6897302 |
Method for synthesizing β-L-5-fluoro-2′,3′-dideoxy-2′,3′-didehydrocytidine (β-L-FD4C)
The invention provides a method of synthesizing β-L-5-fluoro-2′,3′-dideoxy-2′,3′-didehydrocytidine (β-L-FD4C). The method allows for large-scale production of β-L-FD4C in an efficient,...
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6884881 |
2′-Substituted RNA preparation
A process for the preparation of a compound of formula (1):
is provided, which comprises the reaction a compound of formula (2):
with a compound of formula Al(OR) 3 under substantially...
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6884880 |
Process for the preparation of 9-β-anomeric nucleoside analogs
A process for substantially enhancing the regio and stereoselective synthesis of 9-β-anomeric nucleoside analogs is described. The introduction of the sugar moiety onto a 6-substituted purine base...
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6822089 |
Preparation of deoxynucleosides
Methods for preparing deoxynucleosides from their corresponding ribonucleosides by forming 3-tert-butylphenoxythiocarbonylderivatives of the ribonucleosides and subsequently effecting radical...
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6770439 |
Sets of generalized target-binding e-tag probes
Probe sets for the multiplexed detection of the binding of, or interaction between, one or more ligands and target antiligands are provided. Detection involves the release of identifying tags as a...
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6696555 |
3'-Desoxypentopyranosyl nucleic acid, its production and its use
The invention relates to a 3′-deoxypentopyranosylnucleic acid consisting essentially of 3′-deoxypentopyranosylnucleosides of the formulae (I) or of the formulae (II) their preparation and...
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6613894 |
Method for producing a pyranosyl nucleic acid conjugate
The invention relates to a process for the preparation of a pyranosyl nucleic acid of the formula (I) or of the formula (II) The process for the preparation of the pyranosyl nucleic acid...
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6596859 |
Process to prepare pyrimidine nucleosides
A process for the production of a compound of the formula: wherein R 1 is hydrogen, alkyl, C 1 -C 16 substituted alkyl, aryl, substituted aryl, aralkyl, substituted aralkyls, alkenyl,...
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6596858 |
Process for the production of 2-halo-6-aminopurine derivatives
A novel process for preparing 2-halo-6-aminopurine derivatives and their analogs is disclosed. The method comprises halogenation of 2,6-diaminopurine derivatives at the C-2 position in a specific...
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6579976 |
Process for producing 2′,3′-diethyl substituted nucleoside derivatives
There can be provided an excellent industrial process for producing compounds having sugar-moiety hydroxyl groups or halogen atoms reduced in nucleic acids or in derivatives thereof by allowing...
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6559299 |
Preparation and isolation of indolocarbazole glycosides
The present invention relates to a novel process to make indolocarbazole glycosides in high purity which inhibit the growth of tumor cells and are therefore useful in the treatment of cancer in...
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6555677 |
Phase transfer catalyzed glycosidation of an indolocarbazole
The present invention relates to a novel glycosidation process to make intermediates useful in the preparation of indolopyrrolocarbazole derivatives which inhibit the growth of tumor cells and are...
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RE38090 |
3′-substituted nucleoside derivative
The invention relates to a 3′-substituted nucleoside derivative represented by the following general formula (1): wherein B means a nucleic acid base which may have a substituent, Z represents...
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6500946 |
Methods for producing nucleoside derivatives and intermediates therefor
Novel intermediates of nucleoside derivatives, of which the 6-position of the nucleic acid base moiety is substituted with a halogen atom, are produced. Using those novel intermediates, even...
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6437118 |
Vinylating of pyrimidine derivatives
The invention relates to a process for the preparation of vinyl pyrimidines of the formula I wherein R 1 is hydrogen or a carboxylic ester group, and R 2 is hydrogen or a group of the formula...
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6429315 |
Process for preparing N6-substituted adenosine derivatives
This invention is directed to a process for preparing N6-substituted adenosine derivatives, to intermediates useful therefor and to methods of preparing these intermediates.
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6355787 |
Purine nucleoside modifications by palladium catalyzed methods and compounds produced
This invention discloses a method for the preparation of 2′-modified nucleosides, using a palladium catalyst and an alkene functionalized with a heteroatom. Included in the invention are the...
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6350863 |
3, 4-di(acylamino)phenyl ribofuranosides, 2'-deoxyribofuranosides, and methods of making
Provided is an artificial nucleic acid which has a double-stranded structure made of two oligonucleotides, where the oligonucleotide has in a sugar-phosphate backbone structure thereof a sugar...
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6339151 |
Enzyme catalyzed therapeutic agents
This invention provides a method for identifying potential therapeutic agents by contacting a target cell with a candidate therapeutic agent which is a selective substrate for an endogenous,...
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6313286 |
Nucleoside analogues
Nucleoside analogues containing the degenerate base analogue P and derivatives thereof are provided with reporter moieties preferably comprising signal moieties. The nucleoside analogues are useful...
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6271370 |
Process for the synthesis of nucleoside analogs
The present invention relates to an improved method for synthesizing nucleosides with a low α:β anomeric ratio. The method comprises coupling a protected furanosyl halide and an appropriately...
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6262254 |
8-fluoropurine compounds
An efficient, regiocontrolled approach to the synthesis of 8-fluoropurines by direct fluorination of purines with dilute elemental fluorine, or acetyl hypofluorite, is provided. In a preferred...
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6175005 |
Process for the preparation of cyclic ethers containing an o-silylated hydroxyl group
A process is provided which can easily produce a hydroxyl groups-containing cyclic ether compound in which at least one of the hydroxyl groups except a primary hydroxyl group thereof and its...
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6072051 |
Nucleoside derivatives and process for preparing the same
According to the present invention, provided are novel nucleoside derivatives having antiviral activity, in particular, anti-HBV (anti-Hepatitis-B Virus) activity, represented by general formula...
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6005097 |
Processes for high-yield diastereoselective synthesis of dideoxynucleosides
The present invention relates to methods for substantially enhancing the stereoselective synthesis of β-anomeric nucleoside analogs. In methods according to the present invention, the introduction...
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5962675 |
Chemical syntheses of 2'-O-methoxy purine nucleosides
Several processes for the chemical synthesis of 2'-O-methoxy purine nucleosides are herein disclosed.
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5861503 |
Process for producing 8-fluoropurines
An efficient, regiocontrolled approach to the synthesis of 8-fluoropurines by direct fluorination of purines with dilute elemental fluorine, or acetyl hypofluorite, is provided. In a preferred...
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5831072 |
Process for the preparation of 2'-deoxy-2'-halocoformycins or steroisomers thereof
An object of this invention is to provide a novel process for the synthesis of a 2'-deoxy-2'-halocoformycin having an inhibitory activity against adenosine deaminase in a practically high yield....
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5831045 |
Boronic acid-containing polynucleotides
Modified nucleotides and polynucleotides which are useful in hybridization assays for the detection of target genes are provided. The modified polynucleotides contain at least one boronic acid...
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5817799 |
2'-Fluorofuranosyl derivatives and methods for preparing 2'-fluoropyrimidine and 2'-fluoropurine nucleosides
A method of preparing a 2'-fluoro compound of the formula ##STR1## where B is selected from the group consisting of purines and pyrimidines, both of which may be substituted, comprises reacting a...
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5808047 |
Process for the preparation of 2,2'-anhydro- and 2'-keto-1-(3',5'-di-O-protected-β-D-arabinofuranosyl) nucleosides
A process for the preparation of compounds of the formula: ##STR1## wherein Pg and R are protecting groups and B is a nucleobase. The process uses protected nucleobases to form 2,2'-anhydro...
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5801237 |
Method for the purification of short nucleic acids
Method for the purification of a synthetic oligonucleotide from failure sequences comprising contacting a sample containing the desired oligonucleotide in protected water-soluble form with a...
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5763418 |
3'-substituted nucleoside derivatives
The invention relates to a 3'-substituted nucleoside derivative represented by the following general formula (1): ##STR1## wherein B means a nucleic acid base which may have a substituent, Z...
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5756707 |
Method of making 2'-O-alkyl pyrimidine ribonucleosides
Method for production of 2'-O-derivatized uridine and cytosine RNA synthons comprising derivatizing the 2'-hydroxyl group of a partially protected cytosine ribonucleoside to preferentially produce...
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5756706 |
Processes for the diastereoselective synthesis of nucleoside analogues
The present invention relates to highly diastereoselective processes for production of cis-nucleosides and nucleoside analogues and derivatives in high optical purity, and intermediates useful in...
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5744596 |
Nucleoside analogues and synthetic intermediates
The present invention relates to highly diastereoselective processes for production of cis-nucleosides and nucleoside analogues and derivatives in high optical purity and intermediates useful in...
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5717086 |
Preparation of fluoro-nucleosides and intermediates for use therein
2',3'-Dideoxy-3'-fluorouridines are made by reaction of a corresponding anhydronucleoside with hydrogen fluoride in the presence of an organo-iron compound.
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