C07D223/10

METHOD FOR PRODUCING EPSILON-CAPROLACTAM

The present invention relates to a method of producing ε-caprolactam, the method including the following steps (A) and (B): (A) a step of reacting 5-cyanovaleramide with hydrogen in an aqueous solvent in a presence of a hydrogenation catalyst to obtain a 5-cyanovaleramide hydrogenation reaction mixture; (B) a step of heating the 5-cyanovaleramide hydrogenation reaction mixture at a temperature of 180° C. or higher and 300° C. or lower in an aqueous solvent to obtain ε-caprolactam.

METHOD FOR PRODUCING EPSILON-CAPROLACTAM

The present invention relates to a method of producing ε-caprolactam, the method including the following steps (A) and (B): (A) a step of reacting 5-cyanovaleramide with hydrogen in an aqueous solvent in a presence of a hydrogenation catalyst to obtain a 5-cyanovaleramide hydrogenation reaction mixture; (B) a step of heating the 5-cyanovaleramide hydrogenation reaction mixture at a temperature of 180° C. or higher and 300° C. or lower in an aqueous solvent to obtain ε-caprolactam.

PROCESS AND PLANT FOR THE PRODUCTION OF EPSILON-CAPROLACTAM AND AMMONIUM SULFATE ON INDUSTRIAL SCALE

The invention provides a process and a plant for the production of ε-caprolactam and crystalline ammonium sulfate in an industrial-scale plant, wherein the plant comprises a Beckmann rearrangement reaction section, an ammonium sulfate crystallization section, and one or more heat exchangers configured to transfer heat from the Beckmann rearrangement reaction section to the ammonium sulfate crystallization section and wherein the process comprises the steps of: a) feeding (i) cyclohexanone oxime and (ii) oleum and/or sulfuric acid to the Beckmann rearrangement reaction section b) reacting components (i) and (ii) in the Beckmann rearrangement reaction section to form a reaction mixture comprising ε-caprolactam, whereby heat of reaction is generated; c) discharging the reaction mixture comprising ε-caprolactam from the Beckmann rearrangement reaction section; d) removing partially or fully the heat of reaction generated in the Beckmann rearrangement reaction section by one or more heat exchangers configured to transfer heat from the Beckmann rearrangement reaction section; e) feeding an aqueous liquid comprising ammonium sulfate to the ammonium sulfate crystallization section; f) introducing heat into the ammonium sulfate crystallization section comprising the aqueous ammonium-sulfate-comprising liquid by one or more heat exchangers configured to transfer heat into the ammonium sulfate crystallization section; g) forming ammonium sulfate crystals by evaporative crystallization in the ammonium sulfate crystallization section;
characterized in that h) the heat of reaction removed from the Beckmann rearrangement reaction section in step d) is at least partially or fully transferred to the ammonium sulfate crystallization section in step f).

QUATERNARY HETEROATOM CONTAINING COMPOUNDS

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II):

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comprising treating a compound of Formula (I):

##STR00002##

with a transition metal catalyst and under alkylation conditions as valence and stability permit.

QUATERNARY HETEROATOM CONTAINING COMPOUNDS

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II):

##STR00001##

comprising treating a compound of Formula (I):

##STR00002##

with a transition metal catalyst and under alkylation conditions as valence and stability permit.

Protease Inhibitors for Treatment of Coronavirus Infections

Provided herein are compounds of Formula (I), their pharmaceutically acceptable salts, and their pharmaceutical compositions:

##STR00001##

wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4, R.sup.5, and A are defined in the present disclosure. The compounds are potent inhibitors of the main protease (M.sup.pro) of severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2), and they are useful in treating or preventing COVID-19 in a subject.

Protease Inhibitors for Treatment of Coronavirus Infections

Provided herein are compounds of Formula (I), their pharmaceutically acceptable salts, and their pharmaceutical compositions:

##STR00001##

wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4, R.sup.5, and A are defined in the present disclosure. The compounds are potent inhibitors of the main protease (M.sup.pro) of severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2), and they are useful in treating or preventing COVID-19 in a subject.

Derivatives of piperlongumine and uses thereof

The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3-dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to processes for preparing the same; a pharmaceutical composition and formulation containing a derivative of piperlongumine; and use of the derivatives and analogs for treating cancer.

Derivatives of piperlongumine and uses thereof

The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3-dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to processes for preparing the same; a pharmaceutical composition and formulation containing a derivative of piperlongumine; and use of the derivatives and analogs for treating cancer.

Oxidation catalysts

Disclosed are catalysts comprised of platinum and gold. The catalysts are generally useful for the selective oxidation of compositions comprised of a primary alcohol group and at least one secondary alcohol group wherein at least the primary alcohol group is converted to a carboxyl group. More particularly, the catalysts are supported catalysts including particles comprising gold and particles comprising platinum, wherein the molar ratio of platinum to gold is in the range of about 100:1 to about 1:4, the platinum is essentially present as Pt(0) and the platinum-containing particles are of a size in the range of about 2 to about 50 nm. Also disclosed are methods for the oxidative chemocatalytic conversion of carbohydrates to carboxylic acids or derivatives thereof. Additionally, methods are disclosed for the selective oxidation of glucose to glucaric acid or derivatives thereof using catalysts comprising platinum and gold. Further, methods are disclosed for the production of such catalysts.