Abstract: A process of preparing a radioactive compound containing a fluorine-18 isotope is provided. In one embodiment, the process may comprise forming a [18F] fluoroalkyl triflate by triflating a [18F] fluoroalkyl compound with AgOTf, and forming a [18F] fluoroalkylated radioactive compound through alkylation between the [18F] fluoroalkyl triflate and a radioactive compound precursor having at least one group selected from NH, OH and SH.

Abstract: A method for preparing a substituted 1,4-quinone methide from a 3,5-disubstituted 4-hydroxybenzaldehyde is provided. Also provided is a method to prepare a 3,5-disubstituted 4-hydroxybenzaldehyde from the corresponding 2,6-disubstituted phenol.

Abstract: Improved methods of preparing hypocrellin B from 4,9-dihydroxy-3,10-perylenequinones are described.

Abstract: Organozinc compounds of the type R1—Ar1—ZnY (1) can be reacted with different functionalized aryl halides R2—Ar2—X (2) in the presence of catalytic amounts of Ni or Fe in a polar solvent or solvent mixture to form polyfunctional biaryles of the type R1—Ar1—Ar2—R2 (3). Organozinc compounds of the type (1) can be represented by the transmetallation reaction of functionalized aryl magnesium halides or lithium aryl compounds with e.g. ZnBr2.

Abstract: The present invention provides caffeoylquinic acid derivatives and a method of preparing for the same, and also provides pharmaceutical compositions containing caffeoylquinic acid derivatives, and uses of caffeoylquinic acid derivatives in preparation of a medicament for the treatment or prophylaxis of virus diseases, in particular, uses of respiratory syncytial virus and hepatitis B virus, which has the characteristics of safety, high effectiveness and low toxicity.

Abstract: The invention concerns a new process for the preparation of naphthoquinones, in particular an improved process for the preparation of 2,3-disubstituted 1,4-naphthoquinones, in the trans configuration.

Abstract: The invention is a process of using, as a reducing agent, a 12CaO.7Al2O3 electride containing electrons in a number of 1019 or more and 2.3×1021 cm?3 or less in its cages to subject a carbonyl compound to reductive coupling in a solvent, thereby synthesizing a diol or polydiol. The invention is also a process of reducing a ketone compound in a solvent, thereby synthesizing a secondary alcohol or diketone compound. According to the process of the invention, it is possible to synthesize a diol or polydiol, or a secondary alcohol or diketone compound through simple operations in a short period without using an expensive and harmful metal hydride or metal salt nor limiting the atmosphere for the synthesis to an inert gas atmosphere as in conventional processes.

Abstract: [Problem] To provide an organoboron compound-containing reagent for organic synthesis reactions which undergoes no trimerization with dehydration, does not necessitate activation with a base, and is stable and highly active. [Means for Solving Problems] The reagent for organic synthesis reactions contains an organic triol borate salt represented by any of the general formulae (I) to (III) and general formula (XVI): (wherein R1 represents alkyl, alkenyl, etc.; R2 represents optionally substituted alkyl, alkenyl, alkynyl, etc. or represents hydrogen; m+ represents an alkaline metal ion, phosphonium ion, or given ammonium ion; M2+ represents an alkaline earth metal; X represents halogen or alkoxide; Y represents an alkali metal ion, etc.; A represents optionally substituted methylene; and n represents an integer).

Abstract: The present invention refers to new derivatives of the penta-1,4-dien-3-ones, as well as their processes of preparation. These compounds present strong antitumoral activity and promising antiparasitic action, behaving as almost atoxic by laboratory assays and also by hystopathologic studies. The present invention refers also to a pharmaceutical composition including the referred compounds, method of treatment for cancer and parasitic diseases.

Abstract: A polymer having bis(diphenylphosphino)binaphthyl groups that can be used as a catalyst for an addition reaction, especially an asymmetric 1,4-addition reaction, or a reduction reaction, especially an asymmetric reduction reaction, and that can be easily recovered and recycled. The polymer having the bis(diphenylphosphino)binaphthyl groups is one resulting from repetition of a racemic or optically active 2,2?-bis(diphenylphosphino)-1,1?-binaphthyl compound substituted at 5-position thereof with an unsaturated terminal of one (meth)acryloyl group of a compound having multiple (meth)acryloyl groups, that another 2,2?-bis(diphenylphosphino)-1,1?-binaphthyl compound of a next unit is substituted at 5?-position thereof with an unsaturated terminal of another (meth)acryloyl group of the compound having multiple (meth)acryloyl groups so as to have a molecular weight of 1500 to 10000. The reduction catalyst comprises this polymer and a transition metal.

Abstract: In accordance with aspects of the invention methods of using rhodium hydroquinone catalysts for the conjugate addition of boronic acids are disclosed.

Abstract: The present invention provides a catalyst, which has enough catalytic activity as a transition metal particle catalyst including platinum family and the like, is easily separable from products, is reusable and is easily prepared. To prepare the transition metal cluster catalyst of the present invention, an insoluble complex is prepared by forming a complex between a polymer with nitrogen-containing group, such as pyridinium and ammonium group in the principal chain, and a later transition metal compound; and then reducing the complex with a reductant. The transition metal forms clusters, which are stabilized by the polymers. Namely, the present invention is a transition metal cluster catalyst, wherein transition metal clusters are supported by a polymer, which is obtained by reduction reaction of a complex of a transition metal and a polymer with nitrogen-containing group.

Abstract: The present invention relates to a computer-assisted method of a designing of a tubulin inhibitor comprising: a) determining an interaction between a tubulin protein and a chemical known to bind the tubulin protein by evaluating a binding of the tubulin protein to the chemical known to bind the tubulin protein; b) based on the interaction, designing a candidate tubulin inhibitor; c) determining an interaction between the tubulin protein and the candidate tubulin inhibitor by evaluating a binding of the tubulin protein to the candidate tubulin inhibitor; and d) concluding that the candidate tubulin inhibitor inhibits the tubulin protein wherein the conclusion is based on the interaction of step c). The invention also provides compositions and methods of treatment of diseases with the candidate tubulin inhibitors.

Abstract: The invention is a process of using, as a reducing agent, a 12CaO.7Al2O3 electride containing electrons in a number of 1019 or more and 2.3×1021 cm?3 or less in its cages to subject a carbonyl compound to reductive coupling in a solvent, thereby synthesizing a diol or polydiol. The invention is also a process of reducing a ketone compound in a solvent, thereby synthesizing a secondary alcohol or diketone compound. According to the process of the invention, it is possible to synthesize a diol or polydiol, or a secondary alcohol or diketone compound through simple operations in a short period without using an expensive and harmful metal hydride or metal salt nor limiting the atmosphere for the synthesis to an inert gas atmosphere as in conventional processes.

Abstract: The present invention relates to substituted hydroxyacetophenone derivatives having antiproliferative and antimicrobial properties, to pharmaceutical compositions containing them, as well as to a method of preparing them. Moreover, the hydroxyacetophenone derivatives according to the invention can serve as organic intermediates for the preparation of biologically active compounds.

Abstract: To improve a catalytic activity of a composite oxide, to carry out a reaction in a high yield, and to provide a synthesis reaction catalyst having excellent handling properties and a method of a synthesizing a compound using the same, a synthesis reaction catalyst containing a palladium-containing perovskite-type composite oxide having a specific surface area of 0.5 to 9.5 m2/g is used in Suzuki Cross-Couplings given by the following general scheme (14).

Abstract: A method of making a carbonyl compound comprises contacting a compound comprising a secondary hydroxyl group with a basic metal oxide catalyst at a temperature sufficient to maintain the compound comprising a secondary hydroxyl group in a vapor phase.

Abstract: A process by which an ?-oxocarbonyl compound useful as an intermediate for pharmaceuticals/agricultural chemicals can be industrially advantageously and efficiently produced in a high yield. The process, which is for producing an ?-oxocarbonyl compound represented by the general formula (I) wherein R1 and R2 are as defined in the description, comprises oxidizing an ?-hydroxycarbonyl compound represented by the general formula (II) with oxygen or air in the presence of a carboxylic acid and at least one vanadium compound selected from divanadium pentaoxide, divanadium trioxide, divanadium tetraoxide, ammonium metavanadate, sodium metavanadate, potassium metavanadate, triethoxyoxovanadium, tripropoxyoxovanadium, triisopropoxyoxovanadium, vanadium oxobis(acetylacetonate) and vanadium tris(acetylacetonate).

Abstract: A method for aldol reaction in water, which comprises: reacting an aldehyde with a silyl enol ether in an aqueous medium in the presence of a boronic acid represented by the following general formula (1): R1R2BOH??(1) (wherein R1 and R2 are the same or different hydrocarbon groups that may contain a substituent), a surfactant, and a Brønsted acid is provided. This method for aldol reaction in water uses a catalytic amount of the boron source to give products in high yield and selectivity.

Abstract: A process for preparing benzophenones of the formula I, where X may be chlorine, hydroxyl, methoxy or C1-C6-alkylcarbonyloxy, and Y may be chlorine or bromine, by reacting an acid chloride of the formula II where X and Y are as defined above with 3,4,5-trimethoxytoluene, which comprises carrying out the reaction in the presence of a) an aromatic hydrocarbon as a diluent and b) from 0.01 to 0.2 mol % of an iron catalyst, based on the acid chloride, c) at a temperature between 60° C. and the boiling point of the particular diluent.

Abstract: A biotransformation process for preparing chiral aromatic-hydroxy ketones in high yields is described, using 2-hydroxy-3-oxoacid synthase, such as AHAS or TSAS. Optionally substituted arylaldehydes and -oxoacids react in this process to provide pure enantiomers, useful as synthons in the production of various drugs, an example being (R)-phenylacetyl carbinol.

Abstract: There is provided a process for producing an aromatic compound by Friedel-Crafts reaction product, which comprises reacting an aromatic compound with an ester compound in the presence of a heteropolyacid-containing solid acid catalyst.

Abstract: The invention concerns the use of a solid basic catalyst comprising a hydrotalcite structure wherein part at least of the compensating anions are fluoride anions F? for producing Knoevenagel of Michael condensation reactions. The invention also concerns novel solid basic catalysts comprising a hydrotalcite structure characterized by a Mg/Al molar ratio ranging between 2.5 and 3.8 wherein at least part of the compensating anions are fluoride anions F?, and methods for preparing said novel catalysts.

Abstract: Demethylation of 3?, 4?-dimethoxy or 3?, 4?, 5?-trimethoxy benzoic ester of a phenol is carried out in the presence of an excess of aluminum halide in an organic solvent to get 4?-Hydroxy, 3?-methoxy or 4? hydroxy, 3?, 5?-dimethoxy benzoic acid ester of a phenol. The reaction is also applicable to 3?, 4?, 5?-trimethoxy diaryl ketone and some natural products like reserpine.

Abstract: A process for producing a brominated acetal (represented by the formula 3) includes (a) brominating a trifluoromethyl-substituted acetophenone by Br2 in the presence of an alkylene diol. It is optional to produce a trifluoromethyl-substituted 2-alkoxyacetophenone derivative (represented by the formula 9) by (b) reacting the brominated acetal with a metal alkoxide, thereby converting the brominated acetal into an ether; and (c) hydrolyzing the ether in the presence of an acid catalyst to remove an acetal group from the ether, thereby producing the 2-alkoxyacetophenone derivative. Alternatively, the 2-alkoxyacetophenone can be produced by (a) reacting a trifluoromethyl-substituted phenacyl halide with an acetalization agent, thereby converting the phenacyl halide into an acetal; (b) reacting the acetal with a metal alkoxide, thereby converting the acetal into an ether; and (c) hydrolyzing the ether in the presence of an acid catalyst to remove the acetal group from the ether.

Abstract: The present invention provides methods, products, and compositions for selectively inhibiting the growth of Staphylococcus aureus without preventing the growth of Lactobacillus species. Specifically, the present invention discloses the use of tetrahydroiso alpha acid or hexahydro beta acid at a concentration effective to inhibit the growth of S. aureus without preventing the growth of Lactobacillus. The inhibition of S. aureus in accordance with the present invention thus provides useful methods, compositions and products such as feminine hygiene products for treating the diseases associated with S. aureus infections and infestations, i.e., toxic shock syndrome, without disrupting the normal bacterial flora in the area of its application.

Abstract: The present invention provides a process for preparing an aromatic bromide or aromatic iodide from an aromatic amine derivative using nitrite anion and halodimethylsulfonium halide generated in situ from hydrobromic acid/DMSO or hydriodic acid/DMSO. The process for producing compounds of the formula (1) is disclosed (1) wherein X is bromine or iodine: Y is carbon or nitrogen; R1, R2, R3, R4 and R5 which may be the same or different and are selected independently from the group consisting of a hydrogen, a hologen, a C1-C8 alkyl, a C1-C10 alkoxy, a nitro, a formyl, an aryl, a benzyl, a C2-C10 alkylcarbonyl and an arylcarbonyl, provided that adjacent groups as selected from R1, R2, R3, R4 and R5 may combine to form a ring.

Abstract: The present invention relates to a process for the preparation of bicyclic 1,3-diketone salts of formula I wherein R1, R2, R3 and R4 are each independently of the others hydrogen or C1-C4alkyl; A and E are each independently of the other C1-C2alkylene, which may be substituted once or up to four times by a C1-C4alkyl group, and M+is an alkali metal ion, alkaline earth metal ion or ammonium ion, by oxidation of a compound of formula II to a compound of formula III and subsequent conversion to a compound of formula I either in the presence of a base and a catalytic amount of a cyanide or in the presence of an alkali metal alcoholate or alkaline earth metal alcoholate, and to novel bicyclic enol lactone intermediates of formula III for use in that process.

Abstract: The invention provides methods for treating beta-Amyloid protein-induced disease, pharmaceutical compositions and compounds useful for the same, and the use of these compounds for the manufacture of a medicament for treating the same. More particularly, the invention relates to the use of natural product compounds isolated from turmeric, gingko biloba, and ginger, and synthetic chemical analogues thereof, for the treatment of a beta-Amyloid protein-induced disease.

Abstract: Metal salts of organic acids complexed with ?-diketone compounds are multifunctional complexes useful in the formulation of stabilizers for halogenated resins. These complexes may be used jointly with other low toxicity intermediates, such as zinc or magnesium intermediates, to form effective stabilizers that are non-toxic and exhibit better performance than other known stabilizers, including those containing toxic heavy metals such as cadmium or lead. The complex is prepared utilizing a Claisen condensation reaction and precipitation with water and heptane.

Abstract: The invention relates to a method for producing ketones by reacting boric acid derivates with carbocylic acid anhydrides in the presence of a transition metal catalyst. The carboxylic acid anhydrides can either be used in isolated form or produced from carboxylic acids in a reaction mixture. This method enables the simple embodiment of a multitude of functionalized ketones in a single reaction step.

Abstract: The present invention relates to processes for the synthesis of intermediates useful for the synthesis of estrogen receptor modulators. The process includes new methods for annelating 5-, 6- and 7-membered cycloalkenones onto an indanone.

Abstract: The present invention relates to a process for the preparation of aromatic carbonyl compound with carbonyl group attached to its aromatic ring, particularly relates to a process for the preparation of aromatic carbonyl compound with carbonyl group attached to its aromatic ring, by oxidizing with molecular oxygen the methylene or alcoholic group attached to aromatic ring of an aromatic compound, using a polyoxometallate(s) anion exchanged hydrotalcite catalyst.

Abstract: The present invention relates to heavier halogen atom substituted squaraine based dyes of the formula 1 below where X is a heavier halogen atom and pharmaceutically acceptable derivatives thereof, which can be used in photodynamic therapeutical and industrial applications, and to a process for the preparation thereof.

Abstract: One aspect of the present invention relates to novel reaction conditions that allow the efficient synthesis of diaryl ethers from arenes bearing a leaving group and arenols under relatively mild conditions. Another aspect of the present invention relates to the dramatic effects of acidic activators on Ullmann-type couplings involving electron-poor and/or relatively insoluble substrates.

Abstract: Allyl alcohols are converted into corresponding aldehydes or ketones in a high yield under a mild condition by using an inexpensive aluminum alkoxide as an Oppenauer oxidation catalyst and a hydride acceptor. Thus, there is provided an industrially useful method for converting allyl alcohols to corresponding aldehydes or ketones.

Abstract: The present invention provides a process and apparatus for selectively halogenating a ketone of the formula (I) 1

Abstract: A process for producing substantially optically pure sertraline utilizes chromatographic separation on a solid stationary chiral phase of spherical clay particles having an interlayer containing an optically pure metal-organic complex, and a liquid mobile phase preferably containing at least methyl acetate. The liquid mobile phase is preferably free of acetonitrile. The process is operable at temperatures above 40° C.

Abstract: Metal salts of organic acids complexed with &bgr;-diketone compounds are multifunctional complexes useful in the formulation of stabilizers for halogenated resins. These complexes may be used jointly with other low toxicity intermediates, such as zinc or magnesium intermediates, to form effective stabilizers that are non-toxic and exhibit better performance than other known stabilizers, including those containing toxic heavy metals such as cadmium or lead. The complex is prepared utilizing a Claisen condensation reaction and precipitation with water and heptane.

Abstract: The invention relates to a preparation process for derivatives by catalytic dehydrogenation of dibenzosuberone derivatives.

Abstract: Methods and compositions are provided for the direct catalytic asymmetric aldol reaction of aldehydes with donor molecules selected from ketones and nitroalkyl compounds. The reactions employ as catalyst a Group 2A or Group 2B metal complex of a ligand of formula I, as defined further herein.

Abstract: The present invention relates to a first process for producing a 2,2-bis(fluoromethyl)-6-(perfluoroalkyl)-2H-1-benzopyran-4-carboxylic acid. The first process includes the steps of (a) reacting a 2,2-bis(fluoromethyl)-6-(perfluoroalkyl)-2H-1-benzopyran-4-one with a perfluoroalkanesulfonic acid anhydride in the presence of a base, thereby obtaining a perfluoroalkanesulfonic 2,2-bis(fluoromethyl)-6-(perfluoroalkyl)-2H- 1-benzopyran-4-yl ester; and (b) reacting the benzopyranyl ester with carbon monoxide in the presence of a palladium complex compound and a base, thereby obtaining the carboxylic acid. The present invention further relates to a second process for producing a 2-hydroxy-5-(perfluoroalkyl) acetophenone, which can be a raw material for producing the carboxylic acid.

Abstract: The present invention relates to a process for the preparation of high purity and yield &agr;-asarone, trans 2,4,5-trimethoxy cinnamaldehyde, 2,4,5-trimethoxy-phenyl propionone, from &bgr;-asarone or &bgr;-asarone rich Acorus calamus oil containing &agr; and &ggr;-asarone by hydrogenating, followed by treatment with DDQ with or without solid support of silica gel or alumina in dry organic solvent and &agr;-asarone can also be obtained by treating the hydrogenated product of &bgr;-asarone or &bgr;-asarone rich Acorus calamus with DDQ in an aqueous organic solvent to obtain an intermediate 2,4,5-trimethoxy phenyl propionone, which in turn is reduced with sodiumborohydride to obtain the corresponding 2,4,5-trimethoxy-phenyl propanol and followed by final treatment with a dehydrating agent.

Abstract: A Pd(OAc)2/diazabutadiene system has been developed for the catalytic cross-coupling of aryl halides with arylboronic acids. A combination of the diazabutadiene DAB-Cy (1, N,N′-Dicyclohexyl-1,4-dizabutadiene) and Pd(OAc)2 was found to form an excellent catalyst for the Suzuki-Miyaura cross-coupling of various aryl bromides and activated aryl chlorides with arylboronic acids.

Abstract: A method for oxidizing an alkane, comprising the step of oxidizing said alkane with oxygen in the presence of an aldehyde, a copper-based catalyst and a nitrogen-containing compound. This method may be used to convert alkanes to corresponding alcohols and ketone having pharmaceutical activities, etc.

Abstract: A process for the preparation of &bgr;,&ggr;,&dgr;-unsaturated ketones and/or &agr;,&bgr;,&ggr;,&dgr;-unsaturated ketones by the reaction of an unsaturated alcohol with an enol ether or mixture of enol ethers, with formation of ketals as a by-product, at temperatures of from 50° C. to 200° C., in the presence of an acid catalyst, whereby one or all of the reagents is/are heated to the reaction temperature of from 50° C. to 200° C. before the acid catalyst is added.

Abstract: A process for the production of enantiomerically pure or optically enriched sertraline-tetralone from a mixture containing two enantiomers using continuous chuomatography. The chromatography comprises a liquid mobile phase comprising at least one polar solvent and a solid chiral stationary phase comprising a derivatized polysaccharide that is selected from amylosic, cellulosic, chitosan, xylan, curdlan, and inulan class of polysaccharide.

Abstract: The invention relates to new compounds of the formula (I) in which R is phenyl, C1-4alkyl-, C1-4alkoxy- or halogen-substituted phenyl, naphthyl or an aromatic ring containing heteroatoms; X is O or S; R1 and R2 are each a methyl radical or R1 and R2 together are a C4-8alkylene radical; Y is hydroxyl, C1-12alkoxy, C1-4alkylamino, di-C1-4alkylamino or a piperidine or morpholine ring that is attached by its nitrogen atom; to a process for preparing them and to their use as photoinitiators and/or photosensitizers.

Abstract: A method for the preparation of 1,3-diketones is disclosed wherein the method comprises the steps of: (A) mixing an alkali metal base with a hindered alcohol in an aromatic hydrocarbon solvent; (B) boiling the mixture and azeotropically distilling water formed by the reaction between the base and the alcohol, whereby a solution of a hindered alkali metal alkoxide is formed in situ in the solvent; (C) mixing an ester with the solution of the hindered alkali metal alkoxide in the aromatic hydrocarbon solvent; and then (D) adding a ketone to the mixture.

Abstract: New process for the synthesis of the antiinflammatory drug known as nabumetone that consists in reacting 2-acetyl-5-bromo-6-methoxynaphthalene with an alkyl acetate in presence of an alkaline alcoholate to get 4-(5-bromo-6-methoxy-2-naphthyl)-4-hydroxybut-3-en-2-one that by catalytic hydrogenation in a polar solvent and in presence of a base gives 4-(6-methoxy-2-naphthyl)butan-2-one known as nabumetone.