Abstract: Disclosed are processes for preparing levosalbutamol or the pharmacologically acceptable salts thereof on an industrial scale, using asymmetric hydrogenation as the key step and optionally a special sequence of subsequent steps, using rhodium as catalyst and a chiral bidentate phosphine ligand such as (2R, 4R)-4-(dicyclohexylphosphino)-2-(diphenyl-phosphino-methyl)-N-methyl-aminocarbonyl-pyrrolidine as catalyst system.

Abstract: Novel acetylamino benzoic acid compounds, methods of using and pharmaceutical compositions comprising an acetylamino benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.

Abstract: The invention provides processes for the preparation of cinacalcet hydrochloride crystalline Form I.

Abstract: The present invention provides a medicament comprising a benzene compound useful as an insulin sensitizer, a salt thereof or a hydrate of them and a derivative of them as the active ingredient. Specifically, it provides a benzene compound represented by the following formula, a salt thereof or a hydrate of them. In the formula, X represents 1) a C6-10 aryl group which may have one or more substituents or 2) a 5- to 10-membered heteroaryl group which may have one or more substituents; Y represents a group represented by the formula: (in the above formulae, Ry1, Ry2 and Ry3 are the same as or different from one another and each represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, or a C3-7 cycloalkyl group) etc.

Abstract: The present invention relates to a process for converting a tertiary OH group of an organic compound into a tertiary Cl group of the organic compound by using a solvent selected from the group comprising toluene, o-xylene, m-xylene, p-xylene and mixtures thereof, and thionyl chloride as the chlorinating agent.

Abstract: Processes are provided for producing organchlorosilanes and dipodal silanes in which an organic halide or alkene or chloralkene is reacted with a hydridochlorosilane in the presence of a quaternary phosphonium salt catalyst by providing sufficient heat to effect a dehydrohalogenative coupling reaction and/or a hydrosilylation reaction and venting the reaction to control reaction pressure and to remove gaseous byproducts from the reaction. The processes are preferably continuous using a catalyst in fluid form at reaction pressures not exceeding about 600 psi. The reactions may be carried out substantially isothermally and/or isobarically, for example in a plug flow reactor or continuous stirred tank reactor. The processes may produce novel silylated compounds including 1,2-bis(trichlorosilyl)decane or 1,2-bis(trimethoxysilyl)decane.

Abstract: This invention pertains to certain enzyme (CPG2) activated self-immolative nitrogen mustard prodrugs, which are useful in enzyme prodrug therapy (EPT), such as ADEPT and GDEPT, for the treatment of proliferative conditions, such as cancer, and which have the following formula: wherein: RN is independently C1-7alkyl; X1 is independently —I, —Br, or —Cl; X2 is independently —I, —Br, or —Cl; the group —N(CH2CH2X1)(CH2CH2X2) is independently attached at the 2-position or at the 4-position; each RG is independently —H or an ester substituent; n is independently an integer from 0 to 4; each RP, if present, is independently a phenyl substituent; m is independently an integer from 0 to 4; each RM, if present, is independently a mustard substituent; and pharmaceutically acceptable salts, solvates, amides, and esters thereof.

Abstract: Processes are provided for producing organchlorosilanes and dipodal silanes in which an organic halide or alkene or chloralkene is reacted with a hydridochlorosilane in the presence of a quarternary phosphonium salt catalyst by providing sufficient heat to effect a dehydrohalogenative coupling reaction and/or a hydrosilylation reaction and venting the reaction to control reaction pressure and to remove gaseous byproducts from the reaction. The processes are preferably continuous using a catalyst in fluid form at reaction pressures not exceeding about 600 psi. The reactions may be carried out substantially isothermally and/or isobarically, for example in a plug flow reactor or continuous stirred tank reactor. The processes may produce novel silylated compounds including 1,2-bis(trichlorosilyl)decane or 1,2-bis(trimethoxysilyl)decane.

Abstract: The present invention relates to a process for preparing mono-N-sulphonylated diamines by reacting diamines with sulphonyl halides in the presence of water, base and organic solvents.

Abstract: The present invention relates to amorphous and polymorphic forms of sodium 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoate and their use for facilitating the delivery of active agents, such as insulin, to a target.

Abstract: The present invention provides a novel phosphorus-containing organosilicon compound furnished with performance of an oxaphosphorin compound, a method for producing therefore and a resin composition containing the same, particularly a polyester or polycarbonate resin composition and a coating composition containing the same, characterized by that said phosphorus-containing organosilicon compound has in the molecule a phosphorus-containing group (an X group) bonded to a silicon atom and represented by the following chemical formula (1)

Abstract: The invention relates to a process for the production of an [18F]fluorohaloalkane which comprises treatment of a solid support-bound precursor of formula (I): SOLID SUPPORT-LINKER-SO2—O—(CH2)nX (I) wherein n is an integer of from (1) to (7) and X is chloro, bromo or iodo; with 18F? to produce the [18F]fluorohaloalkane of formula (II) 18F—(CH2)n—X (II) wherein n and X are as defined for the compound of formula (I), optionally followed by (i) removal of excess 18F?, for example by ion-exchange chromatography; and/or (ii) removal of organic solvent.

Abstract: A method for producing (meth)acrolein and/or (meth)acrylic acid by subjecting isobutylene and the like or propylene to a vapor-phase catalytic oxidation with molecular oxygen in the presence of a solid oxidation catalyst in a tubular type of fixed bed reactor, wherein a temperature of a hot-spot zone is sufficiently controlled and (meth)acrolein and (meth)acrylic acid are produced with a high yield. A method for producing (meth)acrolein and/or (meth)acrylic acid by passing a raw material gas comprising isobutylene and the like or propylene and oxygen through a catalyst layer in a tubular type of fixed bed reactor which is filled with a solid oxidation catalyst, which includes passing a gas containing isobutylene and the like or propylene in a concentration lower than that of the raw material gas, and oxygen through the catalyst layer for a period of one hour or more prior to passing the raw material gas through the catalyst layer.

Abstract: A method of producing a near-infrared absorbing dye compound, useful for image forming materials, infrared heat-sensitive recording devices, optical film materials, and the like, containing a process of reacting a compound represented by formula (I) with halogenating agent. wherein R111, R112, R121, R122, R131, R132, R141 and R142 each independently represent a hydrogen atom, an aliphatic group or an aromatic group; R103, R113, R123, R133 and R143 each independently represent a substituent; and n103, n113, n123, n133 and n143 each independently denote an integer from 0 to 4.

Abstract: A guest host assembly comprising a host assembly formed of calixarene molecules and a guest component located within the host assembly. A crystallographic assembly of layers of the calixarene molecules and stacked along the crystallographic c axis of the assembly in a repeating configuration associated together predominantly by van der Waal forces. The guest component is transferable through the host assembly in a direction normal to the stacked layers. The calixarene molecules are configured in bilayers of adjacent layers along the c axis. The bilayers are shifted along the a or b axis so the assembly, relative to a corresponding assembly of the calixarene molecules without the inclusion of the guest component is shifted. The calixarene are calix(N)arenes in which N is an integer within the range of 4–8. The calixarene molecules are distally substituted with a substituent such as methyl, ethyl, propyl, butyl amyl or phenyl groups.

Abstract: Compounds of formula (I) or a salt or solvate thereof, wherein: x represents 0 or 1; y represents 0 or 1; R1 and R2 independently represent —C1-9 alkyleneC1-6 fluoroalkyl, which fluoroalkyl moiety contains at least 1 fluorine atom and not more than 3 consecutive perfluorocarbon atoms and wherein the R1 and/or R2 moiety is optionally interrupted by an ether link, processes for their preparation, use of the compounds in the preparation of pharmaceutical formulations and the formulations are described.

Abstract: A process is proposed for preparing (meth)acrolein and/or (meth)acrylic acid by partially oxidizing C3 and/or C4 precursor compounds in the gas phase in the presence of a heterogeneous particulate catalyst, in a reactor having two or more thermoplates (1) arranged vertically and parallel to each other while in each case leaving a gap (2), the heterogeneous particulate catalyst being installed in the gaps (2) and the gaseous reaction mixture being passed through the gaps (2), which comprises monitoring, controlling and/or regulating the process by selecting as a monitoring, control and/or regulation parameter one or more temperatures which are measured in one or more gaps (2), at one or more measurement points which are distributed over the height of each gap (2).

Abstract: A method of obtaining an enantioenriched organic compound comprising the steps of: 1) generating from a starting racemic, non-enantiopure or achiral compound a first mixture comprising at least one fluorous-tagged compound and at least one other non-fluorous tagged compound, at least one of these two compounds being enantioenriched relative to the starting compound; 2) contacting a first non-fluorous phase including the first mixture with a fluorous phase at a first phase interface, the fluorous-tagged compound distributing between the first non-fluorous phase and the fluorous phase; and 3) contacting the fluorous phase with a second non-fluorous phase at a second phase interface. The method further includes the step of having a third compound in the second non-fluorous phase that reacts with the fluorous-tagged compound to produce a second compound and the step of generating the first mixture by chemical or enzymatic kinetic resolution of a racemic or non-enantiopure compound.

Abstract: This invention is directed to compounds of the following formula: wherein when a is 0, b is 1 or 2; when a is 1, b is 1, m is from 0-3, X is O or S, Y is halogeno, R1 is hydrogen C1-4 alkyl, R2 is hydrogen, C1-4 alkyl, or optionally substituted propargyl and R3 and R4 are each independently hydrogen, C1-6 alkyl, C6-12 aryl, C6-12 aralkyl each optionally substituted. This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADD), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome, Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia. This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: Disclosed is a process in which surface-active additives are used in the slurry phase Direct Synthesis of trialkoxysilanes to shorten the period between the start of the reaction and the attainment of steady-state rates and selectivities, to improve product yields and to control or prevent foam formation. Compositions comprising silicone antifoam compounds and fluorosilicone polymers are the preferred surface-active additives of the instant process.