Abstract: Compounds of the formula in which W is O, S, S(O) or S(O)2; X is —SR4, —S(O)R4, or —S(O)2R4, —S(O)2NR5R6; or X is —C(O)NR5R6 provided that —C(O)NR5R6 is located at the 3′, 4′ or 5′ position; Y is O or H2; Z is hydrogen, halogen, hydroxy, optionally substituted alkoxy, aralkoxy, acyloxy or alkoxycarbonyloxy; R is hydrogen, halogen, trifluoromethyl, lower alkyl or cycloalkyl; R1 is hydroxy, optionally substituted alkoxy, aryloxy, heteroaryloxy, aralkyloxy, cycloalkoxy, heteroaralkoxy or —NR5R6; R2 is hydrogen, halogen or alkyl; R3 is halogen or alkyl; R4 is optionally substituted alkyl, aryl, aralkyl, heteroaralkyl or heteroaryl; R5, R6 and R7 are independently hydrogen, optionally substituted alkyl, cycloalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; or R5 and R6 combined are alkylene optionally interrupted by O, S, S(O), S(O)2 or NR7 which together with the nitrogen atom to which they are attached form a 5- to 7-membered ring;

Abstract: The invention pertains to a process for preparing guaifenesin tannate. The process involves the steps of mixing guaifenesin with tannic acid in the presence of water, continuing to mix the reaction mixture for about 5 minutes to about 4 hours and thereafter removing at least about 80 wt.% of the water by freeze-drying the reaction mixture.

Abstract: Disclosed is a method for the recovery of crystalline terephthalic acid containing less than about 150 ppmw p-toluic acid by subjecting a solution of terephthalic acid containing minor amounts of p-toluic acid to crystallization in a crystallization zone comprising a plurality of series-connected crystallizers wherein the solution is subjected to rate-controlled evaporative cooling by sequential reduction in pressure and temperature to cause crystallization of terephthalic acid, wherein the pressure of the solution at the end of the crystallization zone is about ambient pressure or less. Solvent which is evaporated from the crystallizers is collected and condensed and the condensed solvent is returned to the crystallization zone at a point subsequent to the crystallizer from which it was obtained.

Abstract: The present invention provides the tosylate salt of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol, the monohydrate of such salt, processes useful in the preparation of such salt and such monohydrate, pharmaceutical compositions comprising such salt, or such monohydrate, methods of treating &bgr;3-adrenergic receptor-mediated diseases, conditions, and disorders in a mammal using such salt, such monohydrate, or such pharmaceutical compositions; and methods of increasing the content of lean meat in edible animals using such salt, such monohydrate, or such pharmaceutical compositions.

Abstract: Certain non-nucleoside compounds that will selectively inhibit telomerase by targeting the nucleic add structures, such as G-quadruplexes, that may be associated with human telomeres or telomerase have been identified. Inhibition of human telomerase by two perylenetetracarboxylic acid diimides and a carbocyanine has been demonstrated. 1H-NMR studies have evidenced the stabilization of a G-quadruplex by the perylenetetracarboxylic acid diimide compounds and provided evidence that these and structurally related compounds inhibit the telomerase enzyme by a mechanism consistent with interaction with G-quadruplex structures.

Abstract: 3-(3-Methyl-4-hydroxyphenyl)-3-methylbutyl aldehyde may be produced from 3-(3-methyl-4-hydroxyphenyl)-3-methylbutyric acid by converting the carboxyl group into a formyl group. N-[N-[3-(3-methyl-4-hydroxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester, which is useful as a sweetener having a high potency of sweetness, can be easily and efficiently prepared on an industrial production from such an aldehyde derivative, via a reductive alkylation reaction with aspartame. Therefore, 3-(3-Methyl-4-hydroxyphenyl)-3-methylbutyl aldehyde is extremely excellent as an intermediate for the production of N-[N-[3-(3-methyl-4-hydroxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester.

Abstract: The present invention is a novel intermediate, compound of the formula (VI) and salts thereof. In addition, the invention includes a process for the preparation of a 15(S)-prostaglandin intermediates compounds (IV) and (XVIII) which comprises (1) contacting a the corresponding enone with (−)-chlorodiisopinocampheylborane while maintaining the reaction mixture temperature in the range of from about −50° to about 0° and (2) contacting the reaction mixture of step (1) with a boron complexing agent.

Abstract: Fluorinated multifunctional alcohols containing at least 3 primary hydroxyl groups are disclosed. Such alcohols allow for easy synthesis of multifunctional crosslinkers such as acrylates, epoxies and vinyl ethers. The multifunctional crosslinkers are used in fluorinated optical coating and waveguide compositions to increase curing speed and crosslinking density.

Abstract: Compounds of formula (I), their salts and solvates, wherein the substituents are as described herein, are FKBP inhibitors.

Abstract: The present invention relates to the field of organic synthesis and more specifically to a process for the preparation of Michael-adducts, as defined below, by reacting a &bgr;,&bgr;- or a &agr;,&bgr;-disubstituted, or a &agr;,&bgr;,&bgr;-trisubstituted, &agr;,&bgr;-unsaturated ketone (I) with a &bgr;-ketoester or a &bgr;-diketone (II) in presence of a suitable catalyst of formula M(X)n, according to scheme 1:

Abstract: The present invention relates to a new and industrially advantageous process for the preparation of 3-ethoxy-4-ethoxy-carbonyl-phenyl acetic acid. This compound is a key intermediate for the synthesis of Repaglinide, an oral hypoglycemic agent.

Abstract: A process for the production of acetic acid by reacting carbon monoxide with methanol and/or a reactive derivative thereof in a liquid reaction composition comprising an iridium carbonylation catalyst, methyl iodide, methyl acetate, water and acetic acid characterised in that there is also present in the reaction composition a monodentate phosphine oxide compound in an amount of up to and including 200 mol per gram atom of iridium.

Abstract: 2,3-Dihydrobenzofuran derivatives of general formula (1): wherein R1 represents a hydrogen atom or an acyl group; R2, R3 and R4 represent a hydrogen atom, a lower alkyl group or a lower alkenyl group; R5 and R6 combine to form a cycloalkyl group or a saturated heterocyclic group containing one or more oxygen atoms or sulfur atoms, provided that R2 and R3 can not simultaneously represent a t-butyl group, or optically active isomers or pharmaceutically acceptable salts thereof are useful as therapeutic or prophylactic agents for various renal diseases and as organ preservatives.

Abstract: The invention relates to lower-alkyl esters of 3-(3,4-dihalophenyl)-2,6-dioxopiperidine-3-propionic acid derivatives, and to processes for preparing the same.

Abstract: A process for preparing 3,3-dimethylbutyric acid includes the steps of reacting trimethylpyruvic acid with a first portion of hydrazine to obtain a ketazine, and treating the ketazine with base and a second portion of hydrazine.

Abstract: The subject invention concerns novel analogs of fentanyl opioids. The subject invention also concerns methods for synthesizing the compounds of the invention. The invention also concerns methods for treating pain in a patient by administering a compound of the invention to a person in need of such treatment.

Abstract: The present invention relates to a process to prepare semi synthetic statins, to intermediates formed during said process and to highly purified simvastatin produced by the process.

Abstract: Naphthyl crown ether ligand molecules containing at least two naphthyl groups that are covalently bonded to suitable solid supports and coated by hydrophobic organic solvents are disclosed. These compositions and associated methods are characterized by selectivity of desired amine or amino acid enantiomers over their counter-enantiomers and derivatives. The composition preferably has an &agr;-value greater than or equal to 4. This allows for the separation of such enantiomers with nonchromatographic resin bed separations of three separation stages or less.

Abstract: Novel imidazole derivatives are disclosed. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are useful in the control or treatment of diseases mediated by this receptor.

Abstract: Tocopherol derivatives are provided. In one embodiment, the tocopherol derivative includes a tocopherol moiety covalently coupled to branched hydrophilic moiety. In another embodiment, the tocopherol derivative includes a first tocopherol moiety covalently coupled to a second tocopherol moiety through a hydrophilic moiety. In other embodiments, the derivative includes three or more tocopherol moieties.