Abstract: A process for the formation of a di(hydroxyalkylaryl) aryl phosphate is disclosed which comprises the reaction of an o-alkyl substituted aromatic diol, e.g., an o-alkyl substituted hydroquinone such as o-t-butylhydro-quinone, and monoaryl dihalophosphate, such as monophenyl dichlorophosphate. This process can, in particular, be used to make certain di(hydroxy-o-alkylphenyl) phenyl phosphate compounds, preferably those that are p-hydroxy, such as di(p-hydroxy-o-t-butylphenyl) phenyl phosphate.

Abstract: The present invention provides novel compounds comprising cellular phosphoinositides and analogues tagged with stable or radioactive isotopes. The present invention also provides novel methods for the preparation of the said phosphoinositides by syntheses, and novel key intermediates of synthesis; the novel methods of synthesis are applied also for the preparation of the phosphoinositides in non-labelled form. In addition, the present invention discloses a class of novel compounds as isotope labelled key precursors of labelled phosphoinositides. These precursors are derivatives of the target phosphoinositides, labelled with stable or radioactive isotopes, wherein OH and phosphate groups are blocked with temporary protecting groups.

Abstract: The present invention relates to phosphonic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.

Abstract: The present invention provides an agent for preventing and curing fatty liver containing, as the effective ingredient compound, a carboxylic acid amide derivative represented by the general formula (1), (wherein R is a lower alkyl group; and X is a halogen atom), and a method for curing fatty liver by administering said agent.

Abstract: Improved radioiodinated phospholipid ether analogs are described which exhibit significant tumor avidity and longer plasma half-life relative to shorter chain analogs. Use of these compounds results in superior imaging and visualization of neoplastic lesions and tumor-specific cytotoxic cancer therapy.

Abstract: An &agr;-cyanoacrylate may be formed by first condensing a cyanoacetate with paraformaldehyde or formaldehyde; reacting the polymer formed with an alcohol to transesterify the polymer; and depolymerizing the polymer to form &agr;-cyanoacrylate monomers.

Abstract: The invention relates to a composition of mixed alkylated triphenyl phosphate esters comprising no less than 65% to about 100%, by weight, monoalkylphenyl diphenyl phosphate, up to about 30%, by weight, dialkylphenyl phenyl phosphate, up to about 3%, by weight, trialkylphenyl phosphate, and up to about 5%, by weight, triphenyl phosphate. The alkyl moieties can be isopropyl, isobutyl tertiary-butyl, isoamyl, tertiary-amyl, isooctyl and/or isononyl. The fluids prepared according to the previously described method show unusually low air entrainment values of less than 180 seconds, and as low as 20 seconds, and have a content of triphenyl phosphate that typically varies from about 0 to about 5.0%.

Abstract: A pentavalent phosphorous compound represented by the formula (I): wherein RA forms a cyclic group together with E, O and P, E represents a direct bond or oxygen atom, F represents a connecting group, and RB represents a phenyl group which may be optionally substituted; and the pentavalent phosphorous compound is useful as a stabilizer for an organic material.

Abstract: The present invention relates to novel geranylgeranyl derivatives and the pharmaceutically acceptable salts thereof having antiproliferative activity in eukaryotic cells with respect to the inhibition of protein geranygeranylation. The invention also relates to the pharmaceutical compositions containing the novel derivatives and to the process of preparation thereof.

Abstract: The present invent n provides a method for the preparation of triarylmethyl protecting group reagents. The reagents are prepared from reaction effluent from the cleavage step of oligonucleotide synthetic regimes.

Abstract: A process for preparing alkoxypyrazine derivatives of the general formula: These alkoxypyrazine derivatives are obtained by reacting a glyoxal derivative of the general formula: and an amlinoimidate of the general formula: The alkoxypyrazine derivatives are important intermediates for preparing pharmaceutically active compounds.

Abstract: This invention is directed to an improved process for the preparation of N-(phosphonomethyl)glycine (i.e., “glyphosate”), a salt of N-(phosphonomethyl)glycine, or an ester of N-(phosphonomethyl)glycine. The process comprises combining an N-substituted N-(phosphonomethyl)glycine reactant with oxygen in the presence of a noble metal catalyst. The N-substituted N-(phosphonomethyl)glycine reactant has formula (V): wherein R1 and R2 are independently selected from the group consisting of hydrogen, halogen, —PO3R12R131, —SO3R14, —NO2, hydrocarbyl, and substituted hydrocarbyl other than —CO2R15; and R7, R8, R9, R12, R13, R14, and R15 are independently selected from the group consisting of hydrogen, hydrocarbyl, substituted hydrocarbyl, and an agronomically acceptable cation.

Abstract: A process for the production of liquid meta-rich triaryl phosphate esters having low triphenyl phosphate content and low viscosity comprises (a) an alkylation stage wherein a phenol is reacted with an olefin having 2 to 12 carbon atoms in the presence of a strong acid catalyst to give a reaction product comprising a mixture of meta and para alkylated phenols; and (b) a transalkylation stage wherein the mixture of alkylated phenols from the alkylation stage is heated in the presence of a strong acid catalyst to increase the meta isomer content of the mixture to at least 25% whilst maintaining a phenol level below 22%; and (c) a phosphorylation stage wherein the mixture of alkylated phenols from the transalkylation stage is reacted with a phosphorylating agent; and wherein the strong acid catalyst used in stages (a) and (b) is a Bronsted acid having an acid strength of less than zero. Preferred catalysts are activated clays such as bentonite, montmorillonite or Fullers Earth clay.

Abstract: This invention provides analogues of phosphatidylinositol-phosphates modified at one or more selected inositol-hydroxyls and optionally carrying reporter or anchoring groups attached in the lipid or the inositol residues, and, the synthetic intermediates and methods for the preparation of these analogues. The analogues are useful as research reagents in biomedical studies related to structure, function and therapeuticals, including reference materials for analyzing the metabolic products in safety and efficacy studies of 2- and/or 3-hydroxyl modified inositols and phosphatidylinositols as drug candidates.

Abstract: The present invention relates to a (a) novel dicarboxy alkyl phosphate esters, (b) a method for the preparation of said phosphate ester and (c) application of said phosphate ester in industrial and personal care applications. The compounds of the present invention are made by reacting epoxy succinic acid and a salt of an alkyl phosphate ester under aqueous conditions. The resulting compound is quite stable and offers excellent emulsification properties.

Abstract: The present invention relates to a process for manufacturing substituted triazolinones, which are intermediates in the preparation of herbicidally active compounds. In particular, this invention relates to the reaction of an isothiocyanate with an alkanol to produce a thionocarbamate intermediate product; alkylation of the intermediate product, reaction of the alkylated intermediate with and alkoxycarbobyl or aryloxycarbonyl hydrazine and reaction of the resultant compound with a base to produce a substituted triazolinone. In this context the terms “alkanol” and “alkylation” represent generic terms and thus, include the use of alkanols and alkylating agents having an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkylalkyl group, an aryl group or an arylalkyl group.

Abstract: The invention relates to the preparation of pyrocarbonic acid diesters by an improved process and to the novel pyrocarbonic acid diesters prepared according to said process as well as to the use thereof. The core of the invention is a process for the preparation of a pyrocarbonic acid diester of formula (I) wherein R1 and R1′ are each independently of the other branched or straight-chain C1-C24alkyl, C3-C24alkenyl, C3-C24alkynyl, C4-C12cycloalkyl, C4-C12cycloalkenyl or C7-C24aralkyl, each of which is unsubstituted or substituted by one or more than one substituent which is inert under the reaction conditions, by reacting at least one ester carbonate of formula (II) with 40-50 mol % of a sulfochloride of formula (IV) in the presence of 0.

Abstract: Combination chemical libraries of Formula I and methods for preparation are disclosed. The libraries allow one to screen large numbers of compounds for a desired biological activity with relative ease. The libraries may be tagged or untagged. In preferred libraries, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or substituted piperazinealkanoic acid. The use of the libraries to discover biologically active compounds is also disclosed.

Abstract: A process for the preparation of a substituted aromatic compound in which a chloroaromatic compound and an alkyl-, alkenyl- or aryl-boronic acid ester or anhydride are coupled in the presence of palladium and a lipophilic aliphatic phosphine comprising at least one branched aliphatic group or a lipophilic aliphatic Dis(phosphine). Preferred phosphines include triisopropyl, triisobutyl and tricyclohexylphosphine.

Abstract: A process for producing dialkyl carbonates, such as dimethyl carbonate, from the reaction of a primary alcohol with urea in the presence of a novel organotin catalyst complex with a high boiling electron donor compound acting as solvent which are (1) materials having the general formula RO[CH2(CH2)kCH2O]mR, wherein each R is independently selected from C1-12 alkyl, alkaryl or aralkyl moieties, k=0,1, 2 or 3 and m=1, 2, 3, 4 or 5 and (2) bidentate ligand which form 1:1 bidentate and/or 1:2 monodentate adducts with R′2SnX2(X═Cl, R′O, R′COO or R′COS), R′3SnX, R′SnO, Ph3-nR′SnXn or Ph4-nSnXn (wherein R′=CqH2q-1n=0, 1 or 2 and q=2 1 to 12) and mixtures thereof, such as materials having the general formula RO[CH2(CH2)xCH2O]mR, wherein each R is independently selected from C1-12 alkyl, alkaryl or aralkyl moieties, k=0,1, 2 or 3 and m=1, 2, 3, 4, or 5.