Patent classifications
C07C69/757
PREPARATION METHOD FOR HIGH OPTICAL INDOXACARB INTERMEDIATE
A field of asymmetric catalytic synthesis, and in particular a preparation method for a high optical indoxacarb intermediate includes reacting 5-chloro-2-methoxycarbonyl-1-indanone ester (or indanone ester for short) with an oxidizing agent in the presence of a chiral Zr-salen polymer to obtain an indoxacarb intermediate (2S)-5-chloro-2,3-dihydro-2-hydroxy-1-oxo-1H-indole-2-carboxylic acid methyl ester. The yield is stabilized between 86% and 90%, and the S-enantiomer content is up to 99%. Such catalyst can replace catalysts such as cinchonine, and greatly increase the content of the effective S-enantiomer of the indoxacarb, so that the content of the hydroxyl intermediate S-enantiomer of the indoxacarb is raised from 75% to 99% or more. In addition, the chiral Zr-salen polymer catalyst is recycled without retreatment, and can be recycled at least 5 times or more, greatly reducing the production cost and laying a foundation for the industrial production of high quality indoxacarb.
Compound, resin, resist composition and method for producing resist pattern
Disclosed is a compound represented by formula (I): ##STR00001##
in formula (I), R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a methyl group, X.sup.1 and X.sup.2 each independently represent a group represented by any one of formula (X.sup.1−1) to formula (X.sup.1−8): ##STR00002## A.sup.1 and A.sup.2 each independently represent an aliphatic hydrocarbon group having 1 to 24 carbon atoms which may have a substituent, and —CH.sub.2— included in the aliphatic hydrocarbon group may be replaced by —O—, —S—, —CO— or —S(O).sub.2—, and R.sup.3 represents a hydrocarbon group having 1 to 24 carbon atoms which may have a substituent, and —CH.sub.2— included in the hydrocarbon group may be replaced by —O—, —S—, —CO— or —S(O).sub.2—.
VACCINE ADJUVANTS AND METHODS OF SYNTHESIZING AND USING THE SAME
The disclosure provides compounds useful as adjuvants in vaccines, as well as methods of synthesizing such compounds and methods of using such compounds in the formulation of a vaccine. The disclosure also features methods of administering such vaccines to a subject (e.g., a mammalian subject, such as a human) in order to treat or prevent one or more diseases, such as a disease caused by a viral or bacterial infection.
TRUXILLIC ACID MONOESTER-DERIVATIVES AS SELECTIVE FABP5 INHIBITORS AND PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
The present invention provides a compound, and method of selectively inhibiting the activity of a Fatty Acid Binding Protein (FABP) comprising contacting the FABP with a compound, said compound having the structure:
##STR00001##
TRUXILLIC ACID MONOESTER-DERIVATIVES AS SELECTIVE FABP5 INHIBITORS AND PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
The present invention provides a compound, and method of selectively inhibiting the activity of a Fatty Acid Binding Protein (FABP) comprising contacting the FABP with a compound, said compound having the structure:
##STR00001##
Processes for preparing 5,5-dimethyl-2-oxo-3-cyclopentene-1-carboxylate compounds and 3,5,5-trimethyl-2-oxo-3-cyclopentene-1-carboxylate compounds from 3,3-dimethyl-1-butene-1,4-dicarboxylate compounds and 1,3,3-trimethyl-1-butene-1,4-dicarboxylate compounds, and 1,3,3-trimethyl-1-butene-1,4-dicarboxylate compounds
The present invention provides a process for preparing a compound of the following general formula (2): wherein R.sup.1 represents a monovalent hydrocarbon group having 1 to 10 carbon atoms, and R.sup.3 represents a hydrogen atom or a methyl group, the process comprising: subjecting a compound of the following general formula (1): wherein R.sup.1 and R.sup.2 represent, independently of each other, a monovalent hydrocarbon group having 1 to 10 carbon atoms, R.sup.3 represents a hydrogen atom or a methyl group, and the wavy bond represents an E-configuration, a Z-configuration, or a mixture thereof, to a Dieckmann condensation in the presence of base to form the compound (2). ##STR00001##
Processes for preparing 5,5-dimethyl-2-oxo-3-cyclopentene-1-carboxylate compounds and 3,5,5-trimethyl-2-oxo-3-cyclopentene-1-carboxylate compounds from 3,3-dimethyl-1-butene-1,4-dicarboxylate compounds and 1,3,3-trimethyl-1-butene-1,4-dicarboxylate compounds, and 1,3,3-trimethyl-1-butene-1,4-dicarboxylate compounds
The present invention provides a process for preparing a compound of the following general formula (2): wherein R.sup.1 represents a monovalent hydrocarbon group having 1 to 10 carbon atoms, and R.sup.3 represents a hydrogen atom or a methyl group, the process comprising: subjecting a compound of the following general formula (1): wherein R.sup.1 and R.sup.2 represent, independently of each other, a monovalent hydrocarbon group having 1 to 10 carbon atoms, R.sup.3 represents a hydrogen atom or a methyl group, and the wavy bond represents an E-configuration, a Z-configuration, or a mixture thereof, to a Dieckmann condensation in the presence of base to form the compound (2). ##STR00001##
Hydroxylated tropolone inhibitors of nucleotidyl transferases in herpesvirus and Hepatitis B and uses therefor
The present disclosure relates to inhibitors of herpesvirus nucleic acid metabolism and inhibitors of Hepatitis B virus. Also provided are methods of treatment using these agents.
Hydroxylated tropolone inhibitors of nucleotidyl transferases in herpesvirus and Hepatitis B and uses therefor
The present disclosure relates to inhibitors of herpesvirus nucleic acid metabolism and inhibitors of Hepatitis B virus. Also provided are methods of treatment using these agents.
Carbon-monoxide-releasing molecules and therapeutic applications thereof
Carbon monoxide-releasing organic molecules are described herein. The molecules can be synthesized prior to administration (e.g., ex vivo) or formed in vivo. In those embodiments where the molecules are formed in vivo, reactants are administered under physiological conditions and undergo a cycloaddition reaction to form a product which releases carbon monoxide. In applying such reactions for therapeutic applications in vivo, the cycloaddition and CO release typically occur only under near-physiological or physiological conditions. For example, in some embodiments, the cycloaddition reaction and/or release of carbon monoxide occur at a temperature of about 37° C. and pH of about 7.4. Pharmaceutical compositions and methods for release carbon monoxide are also described.