Patent classifications
C07D313/04
PROCESSES AND INTERMEDIATES FOR PREPARING alpha,omega-DICARBOXYLIC ACID-TERMINATED DIALKANE ETHERS
The present disclosure provides a process for the preparation of compounds of formula (III),
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compounds of formula (V),
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and corresponding salts of formula (IV).
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The compounds made by the methods and processes of the invention are particularly useful for administration in humans and animals.
PROCESSES AND INTERMEDIATES FOR PREPARING alpha,omega-DICARBOXYLIC ACID-TERMINATED DIALKANE ETHERS
The present disclosure provides a process for the preparation of compounds of formula (III),
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compounds of formula (V),
##STR00002##
and corresponding salts of formula (IV).
##STR00003##
The compounds made by the methods and processes of the invention are particularly useful for administration in humans and animals.
CYCLIZATION PROCESSES OF HYDROXYALKENOIC AICDS AND PRODUCTS THEREOF
The invention provides efficient cyclization processes of hydroxyalkenoic acids and products produced therefrom. The following reactions are claimed: Formula (I), (II), (V) and (VI).
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CYCLIZATION PROCESSES OF HYDROXYALKENOIC AICDS AND PRODUCTS THEREOF
The invention provides efficient cyclization processes of hydroxyalkenoic acids and products produced therefrom. The following reactions are claimed: Formula (I), (II), (V) and (VI).
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Hepatitis B antiviral agents
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:
X-A-Y-L-R(I)
which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Hepatitis B antiviral agents
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:
X-A-Y-L-R(I)
which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
BIOORTHOGONAL LINKERS AND REACTIONS
The present disclosure provides bioorthogonal linkers and reagents, including trans-cyclooctene (TCO)- and tetrazine (Tz)-containing compounds. In a general aspect, the present disclosure provides reagents, conjugates, and bioactive molecules containing a trans-cyclooctene (TCO) fragment. Examples of TCO fragments include: Formulae (I) and (II).
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METHOD FOR PREPARING EPSILON-CAPROLACTONE
The present invention discloses a method for preparing -caprolactone. The method comprises the steps of: adding cyclohexanone, a co-oxidant and a certain amount of catalyst into a certain amount of organic solvent, using molecular oxygen as an oxidant, implementing a reaction with stirring for 0.1 to 24 hours under a pressure of 0.1 to 2 MPa and at a temperature of 60 C. to 100 C., wherein the co-oxidant is acrolein, and the catalyst is a carbon material. The present invention has the advantages of high-efficiency co-oxidant, easily available and recovered catalyst, environmental-friendly oxidant, simple operation and low cost.
METHOD FOR PREPARING EPSILON-CAPROLACTONE
The present invention discloses a method for preparing -caprolactone. The method comprises the steps of: adding cyclohexanone, a co-oxidant and a certain amount of catalyst into a certain amount of organic solvent, using molecular oxygen as an oxidant, implementing a reaction with stirring for 0.1 to 24 hours under a pressure of 0.1 to 2 MPa and at a temperature of 60 C. to 100 C., wherein the co-oxidant is acrolein, and the catalyst is a carbon material. The present invention has the advantages of high-efficiency co-oxidant, easily available and recovered catalyst, environmental-friendly oxidant, simple operation and low cost.
MICROORGANISMS AND METHODS FOR THE PRODUCTION OF CAPROLACTONE
The invention provides non-naturally occurring microbial organisms containing caprolactone pathways having at least one exogenous nucleic acid encoding a butadiene pathway enzyme expressed in a sufficient amount to produce caprolactone. The invention additionally provides methods of using such microbial organisms to produce caprolactone by culturing a non-naturally occurring microbial organism containing caprolactone pathways as described herein under conditions and for a sufficient period of time to produce caprolactone.