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: 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 continuous process for manufacturing bisphenol A according to the invention, by reacting phenol and acetone in the presence of a strong acid catalyst and a co-catalyst, is carried out using as co-catalyst a dithio ether of general formula: in which the symbols R and R? each represent a hydrogen atom, an alkyl radical or a phenyl radical, and the symbol R? represents an optionally substituted alkyl radical.

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: The present invention relates to a method of producing a compound represented by the formula [I] or a salt thereof, which comprises reacting a compound represented by the formula [II] or a salt thereof with a compound represented by the formula [III] or a salt thereof, in the presence of a base, in alcohol, and provides a production method of an O-substituted tyrosine compound, which is superior in productivity, versatility and safety, and economically and industrially useful: wherein each symbol is as defined in the specification.

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: Provided is a method for the synthesis of 1,4-dicyclopropyl-1,3-butadiyne from CPA. Such butadiyne is prepared by oxidative coupling of cyclopropyl acetylene (CPA) using catalytic amounts each of copper (I)chloride and tetrametylethylenediamine (TMEDA) in isopropanol under aerobic conditions. The resulting butadiyne can serve as a fuel or a fuel additive for combustion in engines propelling motor vehicles, marine vessels, aircraft, rockets and other vehicles.

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 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: Process for producing an alkyl carboxylate, comprising contacting in an oxidation reaction zone a C2 to C4 alkane, a molecular oxygen-containing gas, the corresponding alkene and optionally water, in the presence of at least one catalyst active for the oxidation of the alkane to the corresponding alkene and carboxylic acid, to produce a first product stream comprising alkene, unreacted alkane, carboxylic acid and water; separating in a first separation means at least a portion of the product stream produced in the oxidation reaction zone into a gaseous stream comprising alkene and unreacted alkane and a liquid stream comprising carboxylic acid and water; and separating by chemical treatment at least a portion of the gaseous stream obtained from the first separation means into respective streams rich in alkene and alkane; wherein the chemical treatment comprises the steps of: (1) contacting the alkene/alkane gaseous stream with a solution of a metal salt capable of selectively chemically absorbing the alkene t

Abstract: The invention relates to a hydroformylation process in which at least one olefin having from 2 to 6 carbon atoms is reacted continuously with carbon monoxide and hydrogen in the presence of a hydroformylation catalyst in a reaction zone in which a liquid phase is present and a stream S) is taken from the liquid phase, heat is removed from this stream and the stream is subsequently returned to the reaction zone without removal of a material component.

Abstract: The present invention is related to pure cis-diiodo-(trans-L-1,2-cyclohexanediamine) Pt (II) complex, and a process of its preparation. The present invention is further related to the preparation of oxaliplatin using said cis-diiodo-(trans-L-1,2-cyclohexanediamine) Pt (II) complex.

Abstract: The present invention relates to a method of saturating ethylene-containing gases with acetic acid before they are fed into a vinyl acetate reactor, in which the acetic acid recovered in the vinyl acetate process is introduced into a column having a countercurrent stripping section and a rectification section and ethylene-containing gas is supplied via the bottom, wherein the liquid taken off at the bottom of the column is divided into two substreams and one substream is pumped back into the column with maintenance of a minimum pumped circulation required for sufficient saturation with acetic acid.

Abstract: The invention includes pharmaceutically active compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for treatment or prophylaxis of undesired thrombosis.

Abstract: Novel perfluoropolyether-modified silanes are improved in water/oil repellency, parting properties, chemical resistance, lubricity, durability, antifouling properties and fingerprint wipe-off. An antireflection filter is also provided comprising an inorganic antireflection layer including a surface layer in the form of a silicon dioxide-base inorganic layer, and an antifouling layer, preferably of the perfluoropolyether-modified silane, on the surface layer. The antifouling layer has a sliding angle of oleic acid of up to 5°, a change of the sliding angle after solvent washing relative to the sliding angle before solvent washing being up to 10%.

Abstract: A method for forming cascade polymers specifically utilizing the amine monomer of the formula The monomer is made by initially reacting nitromethane and CH2?CHCO2-TBu by nucleophilic addition to form the triester nitrotrialkanoate of the formula and then reducing the nitrosubstituent to afford the said amine monomer.

Abstract: This invention describes a reductive amination process whereby perfluorinated ketones or ketals are combined with ?-aminoesters under basic conditions to form metal carboxylates. Diastereoselective reductions of the metal carboxylates enable access to two diastereomers, depending on the reducing conditions.

Abstract: In the production of glycidyl methacrylate from an alkali metal salt of methacrylic acid and epichlorohydrin, at least one water-soluble polymerization inhibitor is added at an appropriate stage of the production. The addition of the water-soluble polymerization inhibitor prevents the formation of insoluble solid matters to increase the efficiency of phase separation in the washing operation for removing a by-produced salt and form a clear interface between the phases, thereby minimizing the recovery loss. In addition, the troubles such as clogging of pipe lines of production apparatus and equipment for waster water treatment can be avoided.

Abstract: The compounds represented by the formula (I) are produced by reacting benzene compound of the formula (IV) or (V) with alkenylidene diacetate of the formula (VI) in the presence of a catalyst comprising one or more members selected from (a) halogenated boron compounds, (b) triflate compounds of Group 11 elements, (c) halogenated compounds of Group 12 elements, and (d) triflate and halogenated compounds of tin and atomic numbers 58 and 66 to 71 elements. R1, R2=H or C1–C10 alkyl group A=Substituted phenyl group corresponding to a compound of formula (IV) or (V), R3, R4=H or C1–C4 alkyl group, m=0 or 1–4, n=1 to 5, k=1 or 2.

Abstract: A simple, high-yield process for making menthyl lactate (ML) is disclosed. Menthol and lactic acid react to produce a mixture comprising menthyl lactate and one or more higher lactoyl esters of ML. Hydrolysis of the esterification mixture follows in the presence of aqueous base under conditions effective to convert the higher lactoyl esters to menthyl lactate. Coincidentally, the conditions minimize hydrolysis of menthyl lactate to menthol, thereby maximizing the overall yield of ML.