Abstract: Methods for preparing phosphonium salts by reacting a primary phosphine or a secondary phosphine with an ester compound selected from the group consisting of: a phosphate triester; a phosphonate diester; a sulfate diester; and a sulfonate ester; to form a phosphonium salt of formula VII wherein each of RQ, RX, RY, and RZ is independently hydrocarbyl and X? is a phosphate, phosphonate, sulfate, or sulfonate are provided herein. These phosphonium salts may find utility in a wide range of applications, including as surfactants, as polar solvents (ionic liquids), as antimicrobial agents, and as a component of spinning finish in polyamide fiber processing.

Abstract: The invention provides a non-aqueous electrolyte solution containing a phosphonosulfonic acid compound represented by formula (I): wherein, in formula (I), R1, R2 and R3 each independently represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a haloalkyl group having 1 to 6 carbon atoms, a phenyl group, a benzyl group, or a group represented by formula (II); R4 and R5 each independently represent a hydrogen atom, a halogen atom, or an alkyl group having 1 to 6 carbon atoms; and n represents an integer from 1 to 6; and wherein, in formula (II), R6, R7 and R8 each independently represent an alkyl group having 1 to 6 carbon atoms, a phenyl group, or a benzyl group; m represents an integer from 0 to 2; and * represents a position of bonding with the oxygen atom in formula (I).

Abstract: The disclosure describes methods of synthesis of phosphonate ester derivatives. Preferred methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of phosphonate ester derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of phosphonate ester derivatives.

Abstract: The invention relates to a novel synthesis method for forming superacid functional molecules that include monomers, as well as new polymers and copolymers formed from the monomers, and uses for these superacid molecules, polymers, and copolymers. The superacid molecules have an alpha,alpha-difluorosulfonic acid functionality that can be obtained by a reaction between various Grignard reagents and an alkyl(2-fluorosulfonyl)-1,1-difluoroacetate, such as methyl(2-fluorosulfonyl-1,1-difluoroacetate. The molecules, polymers and copolymers would be expected to have enhanced ion conductivity, and would be useful in a variety of applications, including as ion-conductive materials, surfactants, and ion exchange resins.

Abstract: Pantoic acid ester neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs exhibiting enhanced oral bioavailability and methods of using acamprosate prodrugs to treat neurodegenerative disorders, psychotic disorders, mood disorders, anxiety disorders, somatoform disorders, movement disorders, substance abuse disorders, binge eating disorder, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis, and pain are disclosed.

Abstract: Reagents useful for attaching biomolecules (e.g., proteins, oligonucleotides, and other biomolecules) to a surface, processes of attaching molecules to a surface to form modified surfaces using these reagents, and methods of detecting a target compound using these modified surfaces are disclosed.

Abstract: The invention relates to methods of preparing compounds of formula (II) wherein Z represents —OR1 or N(R2)R2a—, where R1 is lower alkylene (C1-C6), R2 is lower alkyl or H and R2a is lower alkylene (C1-C6) or H; Q is absent when R2a is H and is otherwise selected from the group consisting of H, —OH and protected forms of —OH; one of X and Y is halogen and the other is —OSO2R3, where R3 is selected from the group consisting of lower alkyl (C1-C6), phenyl and CH2phenyl. The method comprises the steps of: (a) reacting a compound of formula (I) with aziridineethanol or a 2-[(2-haloethyl)amino]ethanol in the presence of a metal halide, to form a compound of the formula (III) wherein one of X and E is halogen and the other is hydroxy, and (b) reacting the compound of formula (III) with an alkyl- or arylsulfonyl halide or alkyl- or arylsulfonyl anhydride to obtain a compound of the formula (II).

Abstract: A quaternary onium aromatic sulfonate represented by the formula: wherein each R1 independently comprises substituted or unsubstituted, aliphatic or aromatic, hydrocarbyl, carbocyclic or heterocyclic radicals, each X is selected from the group consisting of phosphorus and nitrogen; wherein “a” has a value of 0, 1 or 2, and “b” has a value of 0 or 1 with the proviso that (a+b) is equal to 1 or 2; G1 is an aromatic group; E comprises a bis(carbonyloxyalkyl) polydiorganosiloxane, a bis(carbonyloxyaryl) polydiorganosiloxane, and an ether linkage; each Y1 independently comprises hydrogen, a monovalent hydrocarbon group, alkenyl, allyl, halogen, bromine, chlorine; nitro; and OR, wherein R is a monovalent hydrocarbon group; “q” represents any integer from and including zero through the number of positions on G1 available for substitution; “t” represents an integer equal to at least one; “s” represents an integer equal to either zero or one; and “u” represents any integer including zero; with the proviso that whe

Abstract: Reagents useful for attaching biomolecules (e.g., proteins, oligonucleotides, and other biomolecules) to a surface, processes of attaching molecules to a surface to form modified surfaces using these reagents, and methods of detecting a target compound using these modified surfaces are disclosed.

Abstract: Phosphinines of formula (I) can be combined with metal salts to prepare hydroformylation catalysts. The phosphinine complexes have two phosphorus centers that may be substituted with a variety of hetero atoms or alkyl substituents to modify the ligand characteristics of the phosphinine. Phosphinine metal complexes are employed under normal hydroformylation reaction conditions. The preparatory routes to the phosphinine ligands of formula (I) allow for their convenient synthesis.

Abstract: A process for recovering and purifying substituted benzenesulfonates, by neutralizing a mixture including at least one substituted benzenesulfonate, or at least one corresponding substituted benzenesulfonic acid, and sulfur trioxide, sulfuric acid and/or hydrogen chloride in free or bound form, in an aqueous phase using an alkali metal hydroxide, and purifying it in this aqueous phase, and by subsequently separating the substituted benzenesulfonate(s) from this aqueous phase. The mixture is comminuted into particles having a Sauter mean diameter in the range from 1 &mgr;m to 2 cm, either before or during introduction into this aqueous phase.

Abstract: Phosphinines of formula (I) can be combined with metal salts to prepare hydroformylation catalysts. The phosphinine complexes have two phosphorus centers that may be substituted with a variety of hetero atoms or alkyl substituents to modify the ligand characteristics of the phosphinine. Phosphinine metal complexes are employed under normal hydroformylation reaction conditions. The preparatory routes to the phosphinine ligands of formula (I) allow for their convenient synthesis.

Abstract: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalenesulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.

Abstract: Using the process according to the invention, it is possible to provide, with few reaction steps, a novel route to &agr;-substituted ring systems, which optionally have further substituents.

Abstract: Isophosphoramide mustard analogs useful for treating cancer are provided.

Abstract: A process for the preparation of protected dihydroxypropyl trialkylammonium salts, particularly in chiral form is described. In particular, a process for the preparation of (2,2-dimethyl-1,3-dioxolan-4-ylmethyl)trialkylammonium salts, particularly in chiral form is described. Furthermore, a process is described wherein the (2,2-dimethyl-1,3-dioxolan-4ylmethyl)trialkylammonium salts is a 2,2-dimethyl-1,3-dioxolan-4-ylmethyl trimethylammonium salt, preferably in chiral form. The protected dihydroxypropyl trialkylammonium salts lead to L-carnitine (9) when in chiral form (5).

Abstract: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalenesulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.

Abstract: The present invention relates to phosphonsulfonates and the pharmaceutically-acceptable salts and esters thereof, having the following structure according to formula (I): ##STR1## The present invention further relates to pharmaceutical compositions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients. Finally, the present invention relates to methods for treating or preventing pathological conditions characterized by abnormal calcium and phosphate metabolism in humans or other mammals, including treating or preventing osteoporosis and arthritis, especially rheumatoid arthritis and osteoarthritis. This method comprises administering to a human or other mammal in need of such treatment of a safe and effective amount of a compound or composition of the present invention.

Abstract: .alpha.-Phosphonosulfonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is H, alkyl, arylalkyl or aryl; R4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.

Abstract: A method for making a substituted benzene compound includes reacting a 2-substituted benzenesulfonate or the 2-substituted benzenesulfonate further substituted in the 3, 4 or 5-position with a lithium compound to form an intermediate; and reacting the intermediate with an electrophile to form a 2,6-disubstituted benzenesulfonate or a 2,6-disubstituted benzenesulfonate further substituted in the 3, 4 or 5-position.

Abstract: A series of compounds of Formula I which have anti-tumor activity, and are useful in treating viral infections, their compositions and use. ##STR1## In Formula I B is a purine or pyrimidine base; alk.sub.1 alk.sub.2 and alk.sub.3 are chemical bonds or alkylene groups; Q is hydrogen or hydroxyl; and R.sub.1 -R.sub.4 are hydrogen or alkyl.

Abstract: This invention pertains to phosphosulfonates, having the general formula ##STR1## wherein Y is phenyl, naphthyl, benzyl, a (C.sub.5 -C.sub.8)cycloalkyl, a 5-membered heteroaromatic ring, a 6-membered heteraromatic ring, a fused 5,6-membered heteroaromatic ring, or a fused 6,6-membered heteroaromatic ring; andX is oxygen or sulfur; andR.sup.1 and R.sup.2 are each independently selected from substituted or unsubstituted alkyl, alkoxy, alkylthio, alkenyloxy, alkynyloxy, haloalkoxy, cyanoalkoxy, alkoxyalkoxy, cycloalkyloxy, cycloalkylalkoxy, alkylideneiminooxy, chloro, amino, phenyl or phenoxy; or R.sup.1 and R.sup.2 are both alkoxy, taken together with the phosphorus atom to form a 6-membered oxygen-containing ring; compositions containing these compounds and their use as herbicides.

Abstract: The present invention relates to fluorinated carboxylic acid esters of phosphono- and phosphinocarboxylic acids containing hydroxyl and/or mercapto groups, their use as waterproofing and/or oil-repellency agents, and a method for their preparation.

Abstract: The present invention relates to fluorinated carboxylic acid esters of phosphonocarboxylic acids containing acrylate and/or methacrylate groups, their use as waterproofing or oil-repellency agents, and a method for their preparation.

Abstract: The present invention relates to a synthetic method of optically active starting materials for various medicaments, which are represented by Formula (I): ##STR1## wherein R.sup.1 is hydrogen or hydroxy protecting group; * is an asymmetric carbon; R.sup.2 ' is hydrogen or an optionally substituted lower alkyl; and Q is --CH.dbd.P(Ph).sub.3, --CH.sub.2 P(O)(OMe).sub.2, or --CH.sub.2 S(O)Me, in high optical purity on a large scale.In more detail, the present invention provides intermediates and a method for the production thereof for synthesizing optically active compounds which are able to inhibit activities of HMG-CoA reductase and are, therefore, useful for inhibition of cholesterol biosynthesis.

Abstract: The invention relates to new compounds, di(2-propyl) esters of (R)-, (S)- and (RS)-1-fluoro-2-phosphonomethoxy-3-p-toluenesulfonyloxypropane and the method of producing them. The compounds can be used with advantage in the preparation of N-(3-fluoro-2-phosphonomethoxypropyl) derivatives of heterocyclic purine and pyrimidine bases that have antiviral activity.

Abstract: The present invention relates to fluorinated carboxylic acid esters of phosphonocarboxylic acids or phosphinocarboxylic acids, and the use thereof as surface-active agents.

Abstract: The chemical compound 3,4-dimethyl-2,5,6-tris(p-sulfonatophenyl)-1-phosphanorbernadiene, a process for the preparation thereof and a process for the hydroformylation of olefinically unsaturated compounds with the use of catalysts which contain the aforementioned chemical compound.

Abstract: This invention pertains to phosphosulfonates, having the general formula ##STR1## wherein Y is phenyl, naphthyl, benzyl, a (C.sub.5 -C.sub.8)cycloalkyl, a 5-membered heteroaromatic ring, a 6-membered heteraromatic ring, a fused 5,6-membered heteroaromatic ring, or a fused 6,6-membered heteroaromatic ring; andX is oxygen or sulfur; andR.sup.1 and R.sup.2 are each independently selected from substituted or unsubstituted alkyl, alkoxy, alkylthio, alkenyloxy, alkynyloxy, haloalkoxy, cyanoalkoxy, alkoxyalkoxy, cycloalkyloxy, cycloalkylalkoxy, alkylideneiminooxy, chloro, amino, phenyl or phenoxy; or R.sup.1 and R.sup.2 are both alkoxy, taken together with the phosphorus atom to form a 6-membered oxygen-containing ring; compositions containing these compounds and their use as herbicides.

Abstract: A process for the detection of substances with hydrolase activity in a sample by mixing the sample with a hydrolase substrate and an oxidising agent, and the evaluating the resultant colour intensity, wherein, as hydrolase substrate, there is used at least one compound of the formula ##STR1## in which R.sup.1 is hydrogen or an alkoxy radical,R.sup.2 is hydrogen or halogen, an amino group or an alkoxy or aralkoxy radical,R.sup.3, R.sup.4, R.sup.5, R.sup.6, which can be the same or different, are hydrogen, halogen, carboxyl, a carbamoyl group, sulpho, an amino groups alkyl, an alkoxy radical, aralkoxy, alkylcarbonyl or alkoxycarbonyl, andX is a glycosyl, phosphate or acyl residue. Optionally R.sup.2 and R.sup.3, R.sup.3 and R.sup.4, R.sup.4 and R.sup.5, and R.sup.5 and R.sup.6 can be joined to form a ring system. At least one of R.sup.1 and R.sup.2 must be hydrogen and at least one of R.sup.1, R.sup.2 and R.sup.3 must not be hydrogen. Compounds in which X is .beta.-galactosyl are new.

Abstract: This invention relates to substituted bicycloheptadione derivatives with high herbicidal activity which are represented by general formula (I) ##STR1## (where R.sup.1 is a lower alkyl group, a phenyl group which may be substituted, an aralkyl group which may be substituted, or a heterocyclic group which may be substituted;R.sup.2 is, same or different, a halogen, an alkoxy group, an alkylthio group, an alkylsulfonyl group, an alkyl group, an alkoxyalkyl group, or an alkoxylcarbonyl group, and n is 0 to 4;R.sup.3 and R.sup.4 are, same or different, hydrogen or a lower alkyl group).

Abstract: Cyclic 1-one-2-ene-3-ol compounds substituted in 2-position by an aroyl or heteroaroyl group bearing a hydrocarbylsulfonyloxy or hydrocarbylsulfonylamino substituent exhibiting herbicidal activity.

Abstract: An antistatic resin composition with transparency contains 90-99.9 wt % of a synthetic resin selected from polycarbonate or polymethyl methacrylate and 0.1-10 wt % of a heat-resistant antistat containing phosphonium sulfonate shown by the general formula (I) below: ##STR1## where A is alkyl group with 1-36 carbon atoms, alkenyl group with 4-24 carbon atoms, phenyl group, phenyl group substituted by alkyl group with 1-18 carbon atoms, naphthyl group or naphthyl group substituted by alkyl group with 1-18 carbon atoms, R.sup.1, R.sup.2 and R.sup.3 are identical, each being an aliphatic hydrocarbon group with 1-8 carbon atoms or aromatic hydrocarbon group, and R.sup.4 is a hydrocarbon group with 1-18 carbon atoms.

Abstract: A process is described for the preparation of intermediates useful in the synthesis of Fosfomycin.More particularly, an enantioselective process is described for the preparation of derivatives of (1S,2S)-1,2-dihydroxypropyl-phosphonic acid of formula ##STR1## wherein R.sub.2 and R.sub.3 have the meanings reported in the specification.

Abstract: Substituted benzoyl-bicycloalkyl-1,1,3-diones and related compounds, intermediates therefor, synthesis thereof, and the use of said diones for the control of weeds.

Abstract: Acidic liquids, such as galvanic electrolyte solutions for metal electroplating, contain a surfactant and a foam inhibiting agent which is a perfluoroalkyl-containing ester of phosphoric acid.

Abstract: Phosphinated or phosphonated sulfonic acid compounds are prepared by a process comprising reacting a hypophosphite salt, such as an alkali metal hypophosphite, with an alkenyl sulfonic acid compound of the formula CH.sub.2 .dbd.C(R)C(O)NH--Z--SO.sub.3 --M.sup.+, wherein Z is a divalent (C.sub.1 -C.sub.18)hydrocarbyl group, R is H or (C.sub.1 -C.sub.7)alkyl and M.sup.+ is H.sup.+, NR.sub.4.sup.+ or an equivalent metal cation, such as an alkali metal cation.

Abstract: Compounds of the formula ##STR1## in which R.sub.1 and R.sub.2 denote alkyl, OH, CF.sub.3 or cyanoethyl, A preferably denotes --COOH, R.sub.3 denotes inter alia alkoxycarbonylalkoxy, fairly high-molecular (>C.sub.12) alkoxy, alkylcarbonylalkoxy or nitrobenzyloxy, are valuable herbicides and growth regulators.

Abstract: The compound (phosphonomethyl)perfluoroalkyl sulfonate can be represented by the formula ##STR1## wherein n is from 0 to 7 and R and R.sup.1 are independently selected from the group consisting of hydrogen, 2-cyanoethyl, monovalent hydrocarbons containing from 1 to 18 carbons, monovalent hydrocarbonoxyhydrocarbons containing from 1 to 18 carbons, halogenated monovalent hydrocarbons containing from 1 to 18 carbons and from 1 to 3 halogens, halogenated monovalent hydrocarbonoxyhydrocarbons containing from 1 to 18 carbons and from 1 to 3 halogens. The compound is useful as an intermediate to prepare amino-phosphorous compounds such as N-phosphonomethylglycine.

Abstract: The invention relates to the new compound (2R)-2-[di(2-propyl)phosphonylmethoxy]-3-p-toluenesulfonyloxy-1-trimethyla cetoxypropane and the method of producing it. The compound may be used for producing (S)-N-(3-hydroxy-2-phosphonylmethoxypropyl) derivatives of the heterocyclic purine and pyrimidine bases of antiviral activity.