C07H1/02

METHYL AND ETHYL NICOTINATE-RIBOSIDE-5-PHOSPHATES, PREPARATION THEREOF AND METHODS OF USE THEREOF
20210388018 · 2021-12-16 · ·

The invention provides a compound of formula (I): (I) wherein R is methyl or ethyl. The invention also provides a process for the preparation of the compound. The invention further provides a method for increasing cell NAD.sup.+ production or improving mitochondrial densities in a cell, wherein the method comprises administering to the cell a compound or salt of the invention.

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METHYL AND ETHYL NICOTINATE-RIBOSIDE-5-PHOSPHATES, PREPARATION THEREOF AND METHODS OF USE THEREOF
20210388018 · 2021-12-16 · ·

The invention provides a compound of formula (I): (I) wherein R is methyl or ethyl. The invention also provides a process for the preparation of the compound. The invention further provides a method for increasing cell NAD.sup.+ production or improving mitochondrial densities in a cell, wherein the method comprises administering to the cell a compound or salt of the invention.

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Reuse and recycling for polymer synthesis

Reagents and solvents used for polymer synthesis are reused or recycled rather than discarded. The outflow from each step of polymer synthesis may be collected separately in one of multiple dedicated containers. Reuse returns the outflow from a step of polymer synthesis back to an input of a polymer synthesizer for subsequent use in that same step. Recycling processes the outflow from one or more steps of polymer synthesis to restore original concentrations or purity levels for use in a later synthesis run. Quality control analysis may determine if outflow collected from a polymer synthesizer is reused or recycled. These techniques reduce reagent cost and waste quantity. These techniques may be used with phosphoramidite or enzyme-based synthesis of deoxyribonucleic acid (DNA).

Reuse and recycling for polymer synthesis

Reagents and solvents used for polymer synthesis are reused or recycled rather than discarded. The outflow from each step of polymer synthesis may be collected separately in one of multiple dedicated containers. Reuse returns the outflow from a step of polymer synthesis back to an input of a polymer synthesizer for subsequent use in that same step. Recycling processes the outflow from one or more steps of polymer synthesis to restore original concentrations or purity levels for use in a later synthesis run. Quality control analysis may determine if outflow collected from a polymer synthesizer is reused or recycled. These techniques reduce reagent cost and waste quantity. These techniques may be used with phosphoramidite or enzyme-based synthesis of deoxyribonucleic acid (DNA).

METHOD FOR PREPARING CANGRELOR TETRASODIUM SALT

The present application relates to a method for prepare a Cangrelor tetrasodium salt, comprising: using N-[2-(methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)sulfonyl]adenosine as a raw material to undergo two steps of reaction to obtain a reaction solution containing the Cangrelor tetrasodium salt; separating and purifying once by C18 silica gel column chromatography so as to obtain a Cangrelor tetrasodium salt pure product. The present application has the advantages of short synthesis route, mild reaction conditions, sufficient reaction, simple operation, high product yield, high purity, and environmental friendliness, and is suitable for large-scale preparation.

Novel Process for Preparing Nucleotide P(V) Monomers
20220194976 · 2022-06-23 ·

The present invention relates to an optimized method for preparing a P(V) monomer of formula (IIIa) or (IIIb) from a nucleoside using DBU as a base at about 0.8 equivalent to nucleoside.

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Novel Process for Preparing Nucleotide P(V) Monomers
20220194976 · 2022-06-23 ·

The present invention relates to an optimized method for preparing a P(V) monomer of formula (IIIa) or (IIIb) from a nucleoside using DBU as a base at about 0.8 equivalent to nucleoside.

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Reagents based on a tertiary amine backbone to introduce chemical functionality in nucleic acids and sequence-controlled polymers

It is provided an achiral, non-nucleosidic backbone for phosphoramidites that can be inserted with high yields in nucleic acid strands and sequence-controlled oligo(phosphodiester)s through solid phase synthesis (SPS) using a DNA synthesizer. From this backbone, platforms with useful chemical handles were synthesized, further functionalized, transformed into phosphoramidites and attached to nucleic acid strands and sequence-controlled oligo(phosphodiester)s. The backbone is based on a tertiary amine with a 3-6 carbon spacer between the central nitrogen and the two external hydroxyls. The spacer has been optimized to increase coupling yields and stability.

MULTIVALENT LIGAND CLUSTERS FOR TARGETED DELIVERY OF THERAPEUTIC AGENTS
20220175934 · 2022-06-09 ·

Targeting ligand clusters, and methods of preparing same, are described. A targeting ligand cluster may include first linkers attached to phenolic hydroxyl groups of gallic acid, and one or more targeting ligands attached to each of the first linkers. The targeting ligand cluster may also include a second linker attached to a carboxylic acid of the gallic acid, and at least one of a protecting group, a phosphoramidite, or an oligonucleotide attached to the second linker.

Methods for the preparation of ribosides

Provided are methods of preparing compounds and pharmaceutical compositions comprising a compound Formula VIII for treating Filoviridae virus infections. In one aspect, the compound of Formula VIII is formed from a reaction mixture comprising the compound of Formula IX, the compound of Formula X, a coupling agent such as magnesium chloride and a non-nucleophilic base such as diisopropylethylamine. The compound of Formula IX can be formed from a compound of Formula V and a cyanating agent. The compound of Formula V can be synthesized from a reaction mixture comprising a deprotonating agent such as phenylmagnesium chloride; a silylating agent such as chlorotrimethylsilane; a coupling agent such as isopropylmagnesium chloride, an additive such as LaCl.sub.3-2LiCl, LaCl.sub.3, CeCl.sub.3, NdCl.sub.3, or YCl.sub.3; a compound of Formula VI; and 7-iodopyrrolo[2,1-f][1,2,4]triazin-4-amine. The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.