Abstract: One aspect of the present invention relates to quinine-based and quinidine-based catalysts. Another aspect of the present invention relates to a method of preparing a chiral, non-racemic compound from a prochiral electron-deficient alkene, comprising the step of: reacting a prochiral electron-deficient alkene with a nucleophile in the presence of a catalyst; thereby producing a chiral, non-racemic compound; wherein said catalyst is a derivatized quinine or quinidine.

Abstract: The invention relates to a method and compounds for the preparation of clevidipine butyrate, a very short acting hypertensive calcium antagonist, as well as the synthesis of these compounds useful for the preparation of clevidipine (also known as clevidipine butyrate). Moreover the invention also discloses polymorphic forms of clevidipine butyrate, useful for the preparation of pharmaceutical compositions, and processes to prepare them.

Abstract: A zwitterionic phosphonium salt of Formula I: wherein n is 0 or 1; R is H or SO3; R? is selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, phenyl, substituted phenyl, benzyl and C1-C10 alkoxy-carbonyl; R? is CX3 when n is O; and X is selected from the group consisting of F, Cl, Br and I. The zwitterionic phosphonium salts are useful reagents for the preparation of alkenes and acetals from the corresponding aldehyde.

Abstract: A method for efficiently producing 4-(hydroxymethylphosphinyl)-2-oxobutanoic acid, useful as a production intermediate of herbicide L-AMPB. The method comprises using a compound represented by the below formula (4): (4) where R1 represents a C1-4 alkyl group, arylmethyl group, or substituted arylmethyl group.

Abstract: The present invention relates to a novel process for preparing ?-arylmethylcarbonyl compound of the formula (III), characterized in that aryl- and heteroarylacetic acids and derivatives thereof of the formula (I) are reacted with ?-halomethylcarbonyl compounds of the formula (II) in the presence of a palladium catalyst, of a phosphine ligand, of an inorganic base and of a phase transfer catalyst, optionally using an organic solvent.

Abstract: Process for the preparation of aromatic and heteroaromatic carboxylic acids, carboxylic acid esters and carboxamides by the reaction of aromatic or heteroaromatic halides R—Xn, in which n=integer from 1 to 6, R=substituted or unsubstituted and aromatic or heteroaromatic radical and X=chlorine, bromine or iodine atom, with carbon monoxide and water, ammonia, alcohols or amines in the presence of bases and zero-valent or divalent palladium compounds and bidentate diphosphanes or complexes of zero-valent or divalent palladium with bidentate diphosphanes, in which use is made of bidentate diphosphanes (R1—)(R2—)P—Y—P(—R3)(—R4) in which R1 to R4=unsubstituted aryl radicals or aryl radicals substituted with at least one radical exhibiting a positive resonance effect or a positive inductive effect, or unsubstituted or substituted cycloalkyl radicals, and Y=hydrocarbon group with a total of 2 to 20 carbon atoms, in which at least one of the carbon atoms carries only one or no hydrogen atom as substituent; except f

Abstract: Provided is a process for making non-phthalate plasticizers, by acylating an aromatic compound with a succinic anhydride to form a keto-acid, and then esterifying the keto-acid with C4-C13 OXO-alcohols to form a plasticizer compound. The aromatic rings of the aromatic compound may also be optionally hydrogenated.

Abstract: The present invention provides a process for preparing pemetrexed disodium and its intermediate, 4-(4-carbomethoxyphenyl)butanal. The process for preparing the intermediate comprises the following steps: condensing methyl 4-bromobenzoate with 3-buten-1-ol; extracting with an organic solvent during the work-up; adding silica gel to decolorize; and evaporating the organic solvent to give 4-(4-carbomethoxyphenyl)butanal. The product obtained by the present process, with a yield of higher than 80%, and a purity measured by GC of higher than 95%, may be directly used in the next bromination reaction for synthesizing pemetrexed disodium without purification. The present process is suitable for industrial production, as the operation is simple and the reagents used are cheap and readily available.

Abstract: The present invention pertains to a process for preparing a compound of Formula I that is achiral, racemic or enantiomerically enriched at the hydroxylation center indicated by * comprising contacting a compound of Formula II with an oxidant selected from oxygen, hydrogen peroxide, peracids or alkyl hydroperoxides in the presence of a zirconium complex, wherein R1, R2 and R3 are as defined in the disclosure. This invention also pertains to zirconium complexes useful in this procedure comprising zirconium and a ligand of Formula III or its enantiomer wherein J, R6 and n are as defined in the disclosure. This invention further pertains to a compound of Formula III or its enantiomer.

Abstract: C-nitroso compound releases nitroxyl ion in blood in a second order reaction.

Abstract: Disclosed are esters and a process for the preparation of the esters represented by formula 1: The process includes reacting an alcohol with a long-chain acid R2COOH or long-chain ester R2COOR4 in the presence of an organic solvent and an enzyme with or without the removal of water.

Abstract: The present application discloses a process for preparing a compound of the general formula R1-M1-Ad.zLiX (I) by reacting a compound R1-A (III) with an element M1 in the presence of lithium salts. The application also discloses a process for preparing a compound of the general formula R1m-M3-Tm.zLiX (II) by reacting a compound R1-A (III) with an M3-containing compound in the presence of lithium salts and in the presence of an elemental metal M2. The metal M3 may be selected from Al, Mn, Cu, Zn, Sn, Ti, In, La, Ce, Nd, Y, Li, Sm, Bi, Mg, B, Si and S.

Abstract: The present invention relates to a process for preparing aldehydes by reacting an ?,?-unsaturated carboxylic acid or a salt thereof with carbon monoxide and hydrogen in the presence of a catalyst comprising at least one complex of a metal of transition group VIII of the Periodic Table of the Elements with at least one compound of the formula (I), where Pn is pnicogen; W is a divalent bridging group having from 1 to 8 bridge atoms between the flanking bonds; R1 is a functional group capable of forming at least one intermolecular, noncovalent bond with the —X(?O)OH group of the compound of the formula (I); R2, R3 are each in each case optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl or hetaryl or together with the pnicogen atom and together with the groups Y2 and Y3 if present form an optionally fused and optionally substituted 5- to 8-membered heterocycle; a, b and c are each 0 or 1; and Y1,2,3 are each, independently of one another, O, S, NRa or SiRbRc, where Ra,b,c are each H or in each c

Abstract: A method for preparing an ?-halo enal or enone from an unprotected propargyl alcohol and an electrophilic halogen source catalyzed by the combination of a gold catalyst complex and a metal co-catalyst complex is disclosed. The method can be further enhanced by addition of an additive that facilitates suppression of a des-halo derivative.

Abstract: A proliferation promoting agent for neural stem cells, which comprises a compound produced by Penicillium sp. CND1007 (FERM BP-10917) or a pharmaceutically acceptable salt thereof, as an active ingredient; a novel compound produced by Penicillium sp. CND 1007 or a pharmaceutically acceptable salt thereof; a method for producing neural stem cells, which comprises culturing a neural stem cells to proliferate the neural stem cells in a presence of the compound produced by Penicillium sp. CND 1007 or a pharmaceutically acceptable salt thereof, and harvesting the neural stem cells from the culture; and the like are provided.

Abstract: Disclosed is a composition and methods of treating a skin condition. The ester includes an ester and a dermatologically acceptable carrier.

Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water.

Abstract: The present invention relates to novel compounds of general formula (I), their regioisomers, tautomeric forms, novel intermediates involved in their synthesis. The present invention also relates to a process of preparing compounds of general formula (I), their regioisomers, their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.

Abstract: The racemic and chiral compounds expressed by common formula 1 and formula 2: wherein the lateral substituents X1, X2, X3, X4, X5, X6, X7 and X8 in the benzene rings represent independently hydrogen and fluorine atoms, bridge group Z represent independently the single bond or COO, CH2CH2, CH2O and OCH2 group, substituent Y represents CH3, or CH2F, CHF2, CF3, C2H5 group, symbols n, m, r and t are independently integers of 1 to 8; symbols p and s signify independently number of 0 to 1 and its orthoconic antiferroelectric long helical pitch mixtures prepared by the methods 1) to the racemic components selected from compounds 1 are added chiral components selected from the compound of formula 1 and/or chiral components selected from the compounds of formula 2 and/or another optically active compounds with high helical twisting power, 2) to chiral compound 1 which helical pitches increases with the temperature increase is added chiral compound 1 which helical pitch decreases with temperature increase.

Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein R1 is CHX2, CX3, CX2CHX2 or CX2CX3; each X is independently Cl or F; Z is optionally substituted phenyl; and Q is phenyl or 1-naphthalenyl, each optionally substituted as defined in the disclosure; comprising contacting a compound of Formula 2 with hydroxylamine in the presence of a base. The present invention also relates to novel compounds of Formula 2, useful as starting materials for the aforedescribed method.

Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R2 to R4, L, Q and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition with the above-mentioned properties.

Abstract: Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.

Abstract: The present invention provides novel compositions suitable for use in an intermolecular photodeprotection reaction scheme. Such compositions include a chromophore compound and a second compound having a photocleavable group bonded to a protected functional group. Novel compounds which can used in intramolecular photodeprotection are also provided. These compounds have a chromophore moiety bonded to a photocleavable group, which itself is bonded to a protected group. The compounds and compositions disclosed herein can be used in two-photon and multi-photon excitation.

Abstract: The present invention relates to synthetic processes for preparation of aminotetralin compounds with kinase inhibitory activity. The invention also provides synthetic intermediates useful in the processes of the invention.

Abstract: Novel ligand compounds having the structural formula (I): in which: Ar is a radical selected from among the radicals of formulae (a)-(c) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine, or, alternatively into cosmetic compositions.

Abstract: The invention provides crystalline solid forms of (S)-4-((2S,3S)-7-carbamoyl-1,1-diethyl-3-methoxy-1,2,3,4-tetrahydronaphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline solid forms.

Abstract: The present invention pertains to a process for preparing a compound of Formula I that is achiral, racemic or enantiomerically enriched at the hydroxylation center indicated by * comprising contacting a compound of Formula II with an oxidant selected from oxygen, hydrogen peroxide, peracids or alkyl hydroperoxides in the presence of a zirconium complex, wherein R1, R2 and R3 are as defined in the disclosure. This invention also pertains to zirconium complexes useful in this procedure comprising zirconium and a ligand of Formula III or its enantiomer wherein J, R6 and n are as defined in the disclosure. This invention further pertains to a compound of Formula III or its enantiomer.

Abstract: Novel trans-1,2-diphenylethylene derivatives are synthesized which can be used to form nanoparticles-monomer-nanomolecule-receptor nanosensors. These trans-1,2-diphenyl-ethylene derivatives are soluble in both water and organic solvents, highly fluorescent and can be synthesized in high yields. The trans-1,2-diphenylethylene derivatives are bonded to a nanoparticle, a nanomolecule bonded to the derivative and a receptor bonded to the nanomolecule to form a nanosensor that can be used to detect chemical and biological agents.

Abstract: A (meth)acrylate ester includes a (meth)acrylate monomer moiety having an ester oxygen, an anthraquinone moiety having a transmittance spectrum producing red light, and a linking group covalently coupled to the ester oxygen and the anthraquinone moiety, the linking group including phenyl, naphthyl, a linear alkyl group having from 2 to about 10 carbons, a branched alkyl group having from 3 to about 10 carbons, a cycloalkyl group having from about 3 to about 20 carbons, or a substituted aromatic group.

Abstract: An improved process for preparing o-chloromethylphenylglyoxylic esters of the formula which comprises converting a compound of the formula by reaction with magnesium into the corresponding Grignard reagent which is then reacted with a compound of the formula to give the compound of the formula which is then cleaved by reaction with a chloroformic ester of the formula CICOOR4 or by reaction with phosgene to give the compound of the formula (I), followed by the isolation of the compound of the formula (I), and also an improved process for preparing (E)-2-(2-chloromethylphenyl)-2-alkoximinoacetic esters of the formula and intermediates for their preparation.

Abstract: The present invention relates to novel ketone compounds, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: There is provided a novel process intermediate represented by the general formula (1) or (2): (where, X represents halogen atom, cyano group or the like, Y represents halogen atom, cyano group or the like, R1 represents C1-C6 haloalkyl group or C3-C8 halocycloalkyl group, R2 represents methyl group, halogen atom, cyano group or the like, m represents an integer of 1 to 5, and n represents an integer of 1 to 4).

Abstract: The invention relates to a process for the preparation of (bis)acylphosphanes of formula I, wherein n and m are each independently of the other 1 or 2; R1 if n=1, is e.g. unsubstituted or substituted C1-C18alkyl or C2-C18alkenyl, or phenyl, R1 if n=2, is e.g. a divalent radical of the monovalent radical defined above; R2 is e.g. C1-C18alkyl, C3-C12cycloalkyl, C2-C18alkenyl, mesityl, phenyl, naphthyl; R3 is one of the radicals defined under R1; the process comprises the steps a) contacting e.g.

Abstract: The present invention relates to substituted pyrrole derivatives, which can be used as 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors. Compounds disclosed herein can function as cholesterol lowering agents and can be used for the treatment of cholesterol-related diseases and related symptoms. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and methods of treating cholesterol-related diseases and related symptoms.

Abstract: The invention provides a uv-curable colored composition, comprising (a) at least one selected ethylenically unsaturated photopolymerizable compound; (b) at least one selected curing agent; and (c) at least one selected colorant.

Abstract: The disclosure relates to novel cycloalkylphenyl-substituted cyclic ketoenols of the formula (I) in which J, X, Y, m and CKE are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the disclosure relates to selective herbicidal compositions comprising, firstly, the cycloalkylphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The disclosure furthermore relates to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.

Abstract: The invention described herein relates to certain pyridazinedione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.

Abstract: A method of providing a fragrant odour to an application, comprising the addition thereto of at least one compound of the formula (I) wherein X and Y are independently selected from the group consisting of —CR1R2R3, —NR4R5 and —OR6, wherein R1 to R5 are selected from H and essentially hydrocarbon moieties that optionally comprise at least one oxygen, nitrogen or silicon atom, and R6 is selected from essentially hydrocarbon moieties that optionally comprise at least one oxygen, nitrogen or silicon atom; and A is an essentially hydrocarbon moiety that optionally comprises at least one oxygen, sulphur, nitrogen or silicon atom, with the proviso that the compound A-CHO is a fragrant aldehyde. The use of these compounds in laundry, household and personal care products confers a long-lasting freshness.

Abstract: There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.

Abstract: Disclosed are esters and a process for the preparation of the esters represented by formula 1: The process includes reacting an alcohol with a long-chain acid R2COOH or long-chain ester R2COOR4 in the presence of an organic solvent and an enzyme with or without the removal of water.

Abstract: There is provided a novel process intermediate represented by the general formula (1) or (2): (where, X represents halogen atom, cyano group or the like, Y represents halogen atom, cyano group or the like, R1 represents C1-C6 haloalkyl group or C3-C8 halocycloalkyl group, R2 represents methyl group, halogen atom, cyano group or the like, m represents an integer of 1 to 5, and n represents an integer of 1 to 4).

Abstract: Carbonyl compounds of the formula (II), wherein R1 and R2 are as defined herein, react in the presence of an amine with carboxylic acid derivatives of the formula (II), wherein R3 and EWG are also as defined herein, to give ?,?-unsaturated compounds of the formula (I) according to the following scheme: It is possible under mild reaction conditions to obtain unsaturated esters with high (E) stereoselectivity. The reaction typically proceeds at room temperature or lower without particular requirements such as inert gas, exclusion of moisture, heat, etc., being made. The only by-products obtained are CO2 and water.

Abstract: The present invention relates to a process for preparing pyrrole derivatives of a class that is effective at inhibiting the biosynthesis of cholesterol in humans, and more particularly to improved synthetic methods for preparing 3,5-dihydroxy-7-pyrrol-1-yl heptanoic acids from 1,4-diketo starting materials. The invention further relates to intermediates in this process formula (I).

Abstract: The present invention pertains to a process for preparing a compound of Formula I that is achiral, racemic or enantiomerically enriched at the hydroxylation center indicated by * comprising contacting a compound of Formula II with an oxidant selected from oxygen, hydrogen peroxide, peracids or alkyl hydropetoxides in the presence of a zirconium complex, wherein R1, R2 and R3 are as defined in the disclosure. This invention also pertains to zirconium complexes useful in this procedure comprising zirconium and a ligand of Formula III or its enantiomer wherein J, R6 and n are as defined in the disclosure. This invention further pertains to a compound of Formula III or its enantiomer.

Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.

Abstract: The present invention relates to a process for preparing a beta-keto ester compound of formula (1), which is an intermediate for the synthesis of quinolone antibiotics. Particularly, the present invention is characterized by the reaction of an organo nitrile compound with a salt of mono-alkyl malonate in the presence of metal salt, and so the reaction is easy to control due to its endothermic nature, and is devoid of lachrymatory reagents with excellent reproducibility. Subsequent in situ hydrolysis in the presence of aqueous acid solution provided the compound of formula (1).

Abstract: The present invention relates to the field of organic synthesis and more particularly to a new process for the preparation of an acetal derivative of an alkyl 3-oxo-2-(2-oxoethyl)-1-cyclopentaneacetate. The invention also relates to a method to use said acetal derivative to prepare intermediates useful for the preparation of perfuming ingredients.

Abstract: The present invention pertains to a process for preparing a compound of Formula I that is achiral, racemic or enantiomerically enriched at the hydroxylation center indicated by comprising contacting a compound of Formula II with an oxidant selected from oxygen, hydrogen peroxide, peracids or alkyl hydroperoxides in the presence of a zirconium complex, wherein R1, R2 and R3 are as defined in the disclosure. This invention also pertains to zirconium complexes useful in this procedure comprising zirconium and a ligand of Formula III or its enantiomer wherein J, R6 and n are as defined in the disclosure. This invention further pertains to a compound of Formula III or its enantiomer.

Abstract: The present invention relates to a method of preparing a phenoxy alkanoic, alkenoic, or alkynoic acid or a salt thereof from a phenoxy containing compound via a dicarboxylate intermediate. The phenoxy alkanoic, alkenoic, and alkynoic acids and salts thereof prepared by this method are suitable for use in composition for delivering active agents via oral or other routes of administration to animals. Furthermore, the present invention relates to phenoxy dicarboxylic acids and their salts for delivering active agents, such as biologically or chemically active agents, to a target.