Abstract: In a process for purifying acrylic acid by crystallization by means of vacuum evaporation, a solution which contains acrylic acid and water and may contain further components is crystallized by means of vacuum evaporation with formation of a liquid phase, consisting of a mother liquor containing more than 10% by weight of water and of the crystals, and a vapor phase, the vapor phase is introduced into a liquid material in a condensation zone with formation of a liquid condensation mixture, and the liquid condensation mixture is recycled at least partly to the condensation zone, the operating conditions in the condensation zone being established so that no solid is precipitated.

Abstract: The present invention pertains to a process for the preparation of an enantiomerically enriched chiral carboxylic acid derivative having the partial formula: C—C—C—COOX wherein X is a cation, comprising formation of a dehydro precursor salt having the partial formula: C═C—C—COOX by reaction of the corresponding precursor acid with an at least substantially stoichiometric amount of base, and asymmetric hydrogenation of the salt in the presence of a transition metal complex of a chiral phosphine ligand.

Abstract: A method for preparing chloromethylphenylacetic acids represented by formula (II): wherein a methylphenylacetic acid represented by formula (I): is reacted with a chlorine gas, in an inert solvent, under the irradiation with light or in the presence of a radical initiator, is disclosed. According to the preparation method, high purity chloromethylphenylacetic acids can be prepared at a high yield, without using toxic sulfuryl chloride as a chlorinating agent, by chlorinating the methyl group of the methylphenylacetic acids at a high selectivity while suppressing by-production of a dichloro form or &agr;-chloro form.

Abstract: A combination of an agent which is a substrate for multidrug resistance related protein (MRP) and an inhibitor of MRP which is a nonsteroidal anti-inflammatory drug (NSAID) or a structural analogue thereof for simultaneous, sequential or separate use for increasing the potency of the substrate. The substrates include anti-cancer drugs and transition metal complexes. The combinations can be used to overcome the resistance to MRP substrates exhibited in many conditions, such as resistance to chemotherapy where patients have developed resistance, especially as a result of MRP over-expression to their chemotherapy.

Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a mammal related to supranormal intracellular enzyme activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound is activated selectively within cells having such supranormal intracellular enzyme activity.

Abstract: A method and a catalyst are described for selective oxidation of aromatic compounds (e.g., benzene and its derivatives) into hydroxylated aromatic compounds (e.g., corresponding phenols). For example, benzene can be converted into phenol with a yield of at least 30-40%, and a selectivity on the basis of benzene of at least 95-97%. The selectivity for this reaction based on N2O is at least 90-95%. Therefore, no substantial N2O decomposition or consumption for complete benzene oxidation to CO+CO2 or other side products occurs. Similar results are obtained with benzene derivatives (e.g., fluorobenzene, difluorobenzene, phenol), although the selectivity is somewhat lower in the case of derivatives (e.g., about 80-85% in the case of fluorosubstituted benzenes). A preferred catalyst for this process is a composition containing a high-silica pentasil-type zeolite (e.g, an HZSM-5 type zeolite) which contains no purposefully introduced additives such as transition or noble metals.

Abstract: Compounds of the structure wherein R and R′ are H, alkyl or aryl and each Z, X, Y and X′ is H, acylamino, acyloxy, alkanoyl, alkoxycarbonyl, amino, alkyl, alkoxy, hydroxy, alkylamino, dialkylamino, arylamino, alkylaryl, diarylamino, halo, carboxyl or cyano; and Z can also be are effective UV blockers.

Abstract: Compounds represented by formula (I), and pharmaceutically acceptacle salts thereof; and their method of preparation are provided. Compounds of the above formula are influenza virus neuraminidase inhibitors and can be used in treating patients infected with influenza virus.

Abstract: Bacterial polysaccharides which are used to produced vaccines are isolated then precipitated with a long chain detergent. The precipitated polysaccharides are soluble in organic solvents and can be further derivatized and processed to form the vaccine.

Abstract: Contraceptive activity as well as anti-viral protection can be provided by contraceptive compositions containing a pyrimidine-based nucleoside or nucleotide exhibiting spermicidal or sperm-immobilizing activity. In one example, the active ingredient contains a thymine ring (e.g. AZT) that has 5-halo, 6-alkoxy substitution. Additional improvements in anti-HIV activity for certain AZT derivatives are seen by providing the pentose ring of AZT with aryl phosphate substitution.

Abstract: Monoester monoacid fluoride of dicarboxylic acid is produced by allowing dicaroxylic acid fluoride represented by the following general formula: FOCCF(CF3)OCF2(A)p(CF2)qCOF where A is a bifunctional perfluorinated group having 1 to 10 carbon atoms; p is 0 or 1; and q is 0 or an integer of 1-10, to react with an alcohol having at least 3 carbon atoms, thereby esterifying the terminal CF2COF group. Such selective monoesterification reaction is effective for separation and purification of a dicarboxylic acid difluoride isomer mixture comprising symmetrical dicarboxylic acid difluoride and asymmetrical dicarboxylic acid difluoride.

Abstract: The use of G-block polysaccharides as a modulator for the rheology in a mixture in which a gelling, water-soluble polysaccharide is a component to give the final product a changed viscosity, stability, elasticity, rigidity or similar.

Abstract: A catalytic system for cellulose acylation includes an adduct of sulfuric acid with N,N-dimethylacetamide, free sulfuric acid or free N,N-dimethylacetamide with the following mole ratio of the components: adduct:1.0; free sulfuric acid, max:0.49; or free N,N-dimethylacetamide, max:0.4. A process for producing such a catalytic system is based upon reacting sulfuric acid with N,N-dimethylacetamide in an anhydrous medium at a temperature of 0° C.-25° C. with the following mole weight ratio of the components: sulfuric acid:1.0; N,N-dimethylacetamide, max:1.4. A process for cellulose acylation in the presence of this catalytic system incorporates cellulose treatment with acetic acid followed by treatment of the resultant activated cellulose with a lower fatty acid anhydride at a temperature of 10° C.-90° C. in the presence of this catalytic system taken in an amount of 1.5-30.0 wt.

Abstract: A compound of formula (I) wherein R2 represents C1-3 alkyl, halogen or hydrogen; R3 represents a fluorinated straight or branched alkyl group of 1-6 carbon atoms; and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists of the Adenosine A1 receptor.

Abstract: In a process for the catalytic gas-phase oxidation of acrolein to acrylic acid, the reaction gas starting mixture is passed, with an acrolein loading of ≧150 l (s.t.p.)/l.h, over a fixed-bed catalyst which is housed in two spatially successive reaction zones A, B, the reaction zone B being kept at a higher temperature than the reaction zone A.

Abstract: Ester compounds of formula (1) are useful as monomers to form base resins for use in chemically amplified resist compositions adapted for micropatterning lithography. R1 is H or C1-6 alkyl, R2 is an acid labile group, k is 0 or 1, and m is an integer from 0 to 5.

Abstract: Ester compounds of formula (1) are useful as monomers to form base resins for use in chemically amplified resist compositions adapted for micropatterning lithography. R1 is H or C1-6 alkyl, R2 is an unsubstituted or halo-substituted acyl or alkoxycarbonyl group of 1-15 carbon atoms, R3 is an acid labile group, k is 0 or 1, and m is an integer from 0 to 5.

Abstract: The present invention relates to evenly substituted polysaccharide derivatives having the general structure: polysaccharide—O—R wherein polysaccharide—O represents a substituted or unsubstituted polysaccharide unit and R is a substituent of a polysaccharide-OH group having either the structure R=—A—B— or the structure R=—B—, wherein A is a linear polyether chain having the following structure: A=(—D—O—)n wherein D denotes a linear aliphatic branched or unbranched chain having 2 to 12 C atoms, O represents an oxygen atom and n is a number equal to or greater than 1, and B represents a substituted carbamic acid having the structure wherein E denotes a linear or branched aliphatic chain having 1 to 18 C atoms.

Abstract: There are disclosed are a diastereomer salt of formula (1): a process for producing the same, a process for producing optically active 3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid of formula (2′): a novel optically active amine compound of formula (4): a novel optically active amine compound of formula (8): an imine compound of formula (7) or (11):

Abstract: Synthetic processes are provided wherein oligomeric compounds are prepared having phosphodiester, phosphorothioate, phosphorodithioate, or other covalent linkages. Also provided are synthetic intermediates useful in such processes.