Abstract: The invention relates to a process for preparing a carboxylic ester by reacting an aldehyde in the presence of an aluminum alkoxide, wherein the aluminum alkoxide is obtained either by reacting an aluminum hydride with an aldehyde or by reacting a different aluminum alkoxide with a carboxylic ester.

Abstract: Chiral amino compounds, methods of preparation and uses thereof. Tamiflu can be obtained from the said compounds. Multi-substituted chiral tetrahydropyrrolyl amine which can be used as intermediate compounds of medicament can also be produced by the said compounds.

Abstract: A method for synthesizing (phenylalkyloxy)phenyl-oxobutanoic acid compounds is described. The corresponding (phenylalkyloxy)acylphenyl compound is halogenated, giving the alpha haloketone. The halide is displaced by the anion of a di-alkyl malonate to give a substituted malonic ester. Hydrolysis of the ester and decarboxylation of the diacid gives the desired product.

Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.

Abstract: The invention relates to a method for producing a cross-coupling product of a benzenoid dizonium salt according to the general formula (I), wherein the groups R1, R2, R3, R4, and R5 represent hydrogen, halogen, an alkyl, alkenyl, aryl, alkoxy, aryloxy, nitro, cyano, hydroxy, acetyl, and/or diazo groups independently of each, and X represents BF4, Cl, F, SO3CH3, CO2CH3, PF6, ClO2CH3, or CIO4, comprising the following steps: (a) providing a benzenoid amide, which with the exception of the diazo function has the same substituents R1, R2, R3, R4, and R5 as the benzenoid diazonium salt of the general formula (I), and hydrolytically cleaving the amide to form an amine or providing a corresponding amine, (b) diazotizing the amine thus obtained or provided with a nitrite, and (c) subsequently reacting the benzenoid diazonium salt with a coupling partner in the presence of a catalyst to form a cross-coupling product, wherein the coupling parter is represented by the general formula (II), R6, R7, and R8 are the same or

Abstract: The invention relates to a method for carrying out a chemical reaction for producing a target compound by heating in a reactor a reaction medium containing at least one first reactant, such that a chemical bond inside the first reactant or between the first and a second reactant is formed or modified. The reaction medium is brought into contact with a solid heating medium that can be warmed by electromagnetic induction and that is inside the reactor and is surrounded by the reaction medium. Said heating medium is heated by electromagnetic induction with the aid of an inductor and the target bond is formed from the first reactant or from the first and a second reactant and said target bond is separated from the heating medium.

Abstract: In general, the present invention provides a reliable assay for the quantitative determination of p-aminophenol in an aqueous sample. More particularly, the present invention provides a rapid enzyme-based assay for the quantitative determination of acetaminophen in a sample. The assay employs a xylenol chromophore and a catalyst that is preferably a weak oxidizer. The assay provides reliable results in the presence or absence of N-acetylcystiene (NAC) and can therefore be used to monitor acetaminophen levels during NAC treatment. Methods and kits for determining acetaminophen concentration in an aqueous sample are also provided.

Abstract: Absorbable polyurethanes, polyamides and polyester urethanes prepared from at least one compound selected from: or the corresponding diamines or diisocyanates thereof, wherein each X independently represents —CH2COO—, —CH(CH3)COO—, —CH2CH2OCH2COO—, —CH2CH2CH2CH2CH2COO—, —(CH2)yCOO— where y is 2 to 4 or 6 to 24, or —(CH2CH2O)z?CH2COO— where z? is 2 to 24; each Y represents —COCH2O—, —COCH(CH3)O—, —COCH2OCH2CH2O—, —COCH2CH2CH2CH2CH2O—, —CO(CH2)mO— where m is 2 to 4 or 6 to 24, or —COCH2O(CH2CH2O)n— where n is 2 to 24; R? is hydrogen, benzyl or straight-chained or branched alkyl; p is 1 to 4; and Rn represents one or more members selected from H, alkoxy, benzyloxy, aldehyde, halogen, carboxylic acid and —NO2, which is attached directly to an aromatic ring or attached through an aliphatic chain. Absorbable polymers prepared from these compounds are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention and other implantable medical devices.

Abstract: The present invention refers to a process for preparing a compound of general formula (A), as reported in the description, wherein R is a radical of a drug and R1-R12 are hydrogen or alkyl groups, m, n, o, q, r and s are each independently an integer from 0 to 6, and p is 0 or 1, and X is O, S, SO, SO2, NR13 or PR13 or an aryl, heteroaryl group, said process comprising reacting a compound of formula (B) R—COOZ (B) wherein R is as defined above and Z is hydrogen or a cation selected from: Li+, Na+, K+, Ca++, Mg++, tetralkylammonium, tetralkylphosphonium, with a compound of formula (C), as reported in the description, wherein R1-R12 and m, n, o, p, q, r, s are as defined above and Y is a suitable leaving group.

Abstract: A pyridazine compound represented by formula (1): has an excellent plant disease controlling effect.

Abstract: The present invention relates to hydrazide derivatives of Formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such hydrazide derivatives. Said hydrazide derivatives are useful in the treatment of preterm labor, dysmenorrhea, fertility disorders, asthma, hypertension, undesired blood clotting, preelampsia, eclampsia, an eosinophil disorder, undesired bone loss, renal dysfunction, an immune deficiency disorder, ichthyosis, elevated intraocular pressure, infertility, sexual dysfunction, gastric ulcers and inflammatory disorders.

Abstract: Disclosed is a compound of the formula and dimers thereof, wherein R, R2, X and Z are as described herein. The compounds are useful as colorants, particularly in applications such as phase change inks.

Abstract: Conjugates in which polyamine analogs are conjugated to an amino acid are provided, as well as compositions comprising these conjugates. Methods of using these conjugates as anticancer treatments are also provided.

Abstract: In one embodiment, the present application discloses a process for making the compound of the formula:

Abstract: A process for catalyzing asymmetric dihydroxylations of olefins employs an Os(VI) complex as a catalytic intermediate in the formation of chiral vicinal diol products. The process requires a chiral bidentate ligand that favors diol formation in the “second cycle” of asymmetric dihydroxylation.

Abstract: The invention relates to 2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl-5-nitrobenzofuran hydrochloride, to its preparation and to its use as synthetic intermediate, in particular in preparing 2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl)-5-nitrobenzofuran, itself an intermediate for dronedarone.

Abstract: Disclosed are 3,4,5-trisubstituted aryl nitrone compounds and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have formula (I); where R1-R4 are as defined in the specification. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.

Abstract: The present invention provides methods of making 21-[4′-(nitrooxyalkyl)benzoate] corticosteroid derivatives according to the following general reaction scheme: The invention also provides intermediates useful in making such 21-[4′-(nitrooxyalkyl)benzoate] corticosteroid derivatives as well as methods for making such intermediates.

Abstract: The invention relates to the preparation of hydroxybenzoic benzyl esters by reacting benzyl chloride with hydroxybenzoic acids in the presence of one or more amides.

Abstract: A process of reacting a nitroaniline compound of formula (2): with an acid anhydride or acid halide is carried out in the presence of an alkali metal compound or an alkaline earth metal compound to produce an acylnitroaniline derivative. The process further includes the step of reacting the resulting product with a compound of formula (5); R2—Y to produce an N-acylnitroaniline derivative of formula (1): The N-acylnitroaniline derivative of formula (1) is a useful intermediate for the production of pharmaceuticals.

Abstract: Novel 3-aryl propionic acid derivatives and analogs, process and intermediate for their manufacture, pharmaceutical preparations containing them and the use of the compounds in clinical conditions associated with insulin resistance.

Abstract: The present invention relates to novel antimycobacterial compounds and in particular to antimycobacterial compounds comprised of derivatives of phenyl 4-aminosalicylate. This invention further relates to methods for their preparation, to their use as therapeutic agents and to pharmaceutical compositions containing them. The novel methods of the invention yield derivatives of phenyl 4-aminosalicylate on a multi-gram scale and in high purity for subsequent biological evaluation in drug discovery.

Abstract: This invention relates to derivatives of acrylic acid useful as fungicides, to processes for preparing them, to fungicidal compositions containing them, and to methods of combating fungi, especially fungal infections in plants, using them.

Abstract: The invention relates to the preparation of hydroxybenzoic benzyl esters by reacting benzyl chloride with hydroxybenzoic acids in the presence of one or more amides.

Abstract: A process for producing a benzoylacrylic acid derivative (formula 1) in high yield through a small number of steps and a simple purification step. The process comprises reacting 2,4,5-trifluoro-3-methyl-6-nitrobenzoyl chloride with a compound (formula 2) to yield an aminoacrylic acid derivative (formula 1) and then reacting the aminoacrylic acid derivative (formula 1) with an amine derivative represented by R2—NH2, wherein R2 is a cycloalkyl group or the like.

Abstract: The present invention provides a processes, having practical utility, for preparing 2-oxindoles, N-hydroxy-2-oxindoles, or mixtures thereof comprising: catalytically hydrogenating a 2-nitroarylmalonate diester to produce a 2-(N-hydroxyamino)arylmalonate diester, a 2-aminoarylmalonate diester, or mixtures thereof as a first reaction intermediate; cyclizing, by intramolecular aminolysis of one ester group, the first reaction intermediate to produce a N-hydroxy-2-oxindole-3-carboxylate ester, 2-oxindole-3-carboxylate ester, or mixtures thereof as a second reaction intermediate; and hydrolyzing and decarboxylating the remaining ester group of the second reaction intermediate to produce the N-hydroxy-2-oxindole, the 2-oxindole, or mixtures thereof, wherein the cyclization reaction and the hydrolysis and decarboxylation reaction are conducted in situ with the catalytic hydrogenation reaction without isolation of said reaction intermediates.

Abstract: Compounds having the formulas below, where R is H, lower alkyl, or a pharmaceutically acceptable salt, and where R1 represents i-propyl, t-butyl or n-butyl groups, have selective RXR retionoid agonist activity.

Abstract: A new method for producing unsymmetrically substituted fluorenyl compounds, one step of which is the preparation of 2,7-disubstituted fluoren-9-one derivatives via the nucleophilic substitution of a compound of the formula D wherein A′ is selected from the group consisting of —Br, —Cl, —F, —NO2, and —CN; A is selected from the group consisting of —NO2, —CN, —CO2R, —C(O)R, —SO2R, —SO2RF, —C(CN)═C(CN)2 and —CH═C(CN)2; RF is —CpF2p+1, p=from about 0 to about 10; R is an straight, branched or cyclic aliphatic alkyl group having about 1 to 10 carbon atoms, or an aromatic group such as phenyl or naphthyl; and is a carbonyl or a protected carbonyl such as a ketal or thio-ketal such as wherein R′ is —CrH2r+1; R″ is —(CH2)r—; and r is independently 2 or 3, with a nucleophilic reagent in the presence of an aprotic solvent

Abstract: The invention relates to compounds of formula where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, selected from the group consisting of amines, amino acids, peptide, water, hydrogen sulfide, alcohols, and thiols. The invention also relates to arrays and combinatorial libraries of such compounds, and to a method of preparing such compounds.

Abstract: Disclosed are 3,4,5-trisubstituted aryl nitrone compounds and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have the formula: where R1-R4 are as defined in the specification. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.

Abstract: N-(4-carbamimidoyl-phenyl)-glycine derivatives have the formula: 1

Abstract: The present invention provides compounds represented by the following general formula [I] and salts thereof, which are useful as therapeutic agents for glaucoma, wherein R1 is H, lower alkyl or phenyl, and the phenyl can be substituted by lower alkyl, hydroxy, lower alkoxy, halogen, nitro or phenyl; R2 and R3, being the same or different, are H, halogen or lower alkyl; R4 and R5, being the same or different, are H, lower alkyl or carboxyl or ester thereof; and R6 is carboxyl or phosphono or ester thereof.

Abstract: The invention relates to 2-benzoylcyclohexane-1,3-diones of the formula I where R1, R2 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxyalkyl, alkenyl, alkynyl, —OR5, —OCOR6, —OSO2R6, —SH, —S(O)nR7, —SO2OR5, —SO2NR5R8, —NR8SO2R6 or —NR8COR6; R3 is hydrogen, alkyl, haloalkyl, alkenyl or alkynyl; R4 is hydrogen, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, —COR9, —CO2R9, —COSR9 or —CONR8R9; X is oxygen or sulfur; Z is oxygen or NR8; m is 0 or 1; n is 0, 1 or 2; R5 is hydrogen, alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R6 is alkyl or haloalkyl; R7 is alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R8 is hydrogen or alkyl; R9 is alkyl, alkenyl, alkynyl, phenyl or benzyl; R10 is alkyl, haloalkyl, alkenyl or alkynyl; Q is an unsubstituted or substituted cyclohexane-1,3-dione ring which is linked in the 2-position; where m is 1 if R3 is

Abstract: The present invention concerns alkyl esters of &bgr;-amino acid derivatives which are useful in the synthesis of taxol and analogs.

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.

Abstract: A chemical compound having the formula: ##STR1## wherein P.sub.1 is a hydroxyl protecting group, R.sub.1 may be H or electron withdrawing group, R.sub.2 may be H or electron withdrawing group, R.sub.3 may be H or electron withdrawing group, R.sub.4 may be H or electron withdrawing group, R.sub.5 may be H or electron withdrawing group, R.sub.6 may be an alkyl group, an olefinic group, an aromatic group, Ph, PhCH.sub.2, an O-alkyl group, an O-olefinic group, an O-aromatic group, O--Ph, or O--CH.sub.2 Ph.

Abstract: The compounds of formula I ##STR1## wherein: a) X is O, andY is OC.sub.1 -C.sub.4 alkyl; orb) X is O or S, andY is NHCH.sub.3have fungicidal properties and can be used in plant protection for controlling and preventing disease infestation.

Abstract: A process for preparation of 2-(10,11-dihydro-10-oxodibenzo[b,f]thiepin-2-yl)propionic acid (i.e., Zaltoprofen) is performed by subjecting 2-(4-amino-3-carboxy-methylphenyl)propionic acid or its salt to diazotization and subsequent reaction with thiophenol to produce 2-(3-carboxymethyl-4-phenylthiophenyl)propionic acid or its salt, and subjecting the product to cyclization reaction. Other related processes and related compounds are also disclosed.

Abstract: An efficient protocol for the synthesis of taxol, taxol analogs and their intermediates is described. The process incudes the attachment of the taxol A-ring side chain to baccatin III and for the synthesis of taxol and taxol analogs with variable A-ring side chain structures. A rapid and highly efficient esterification of O-protected isoserine and 3-phenylisoserine acids having N-benzyoloxycarbonyl groups to the C-13 hydroxyl of 7-O-protected baccatin III is followed by a deprotection-acylation sequence to make taxol, cephalomanninne and various analogs, including photoaffinity labeling candidates.

Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.

Abstract: This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein: R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is phenyl optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl naphthyl, furanyl, pyridinyl or thienyl and Ar.sup.1 can be optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, tifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; andAr is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.

Abstract: This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein: R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is phenyl is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl, naphthyl, furanyl, pyridinyl or thienyl and Ar.sup.1 can be optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; andAr is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.

Abstract: Taxane derivatives having alternative C2 substituents.

Abstract: Borneol derivatives of formula I ##STR1## in which R.sup.1 to R.sup.5 and X.sup.1 to X.sup.2 are defined in the specification, and the method of making the same.

Abstract: The present invention provides an efficient route to the C-13 side chain of the anti-cancer drug paclitaxel (TAXOL) and its analogs. The process includes the resolution of racemic erythro 2-hydroxy-3-amino-3-phenylpropionamide by diastereomeric crystallization and its conversion via various intermediates to the threo-ethylester and threo-methylester isomers.

Abstract: (Het)aryloxy-, -thio- and -aminocrotonates of the formula I ##STR1## where the substituents have the following meanings: U is oxygen, sulfur or amino;V is oxygen, sulfur, amino or alkylamino;X, Y and Z independently of one another are .dbd.N-- or .dbd.CR.sup.3 --;R.sup.1 and R.sup.2 independently of one another are alkyl;R.sup.3 is hydrogen, cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and haloalkylthio; andR.sup.4 is an organic radical which is bonded to the skeleton directly or via an oxy, mercapto, amino, carboxyl or carbonylamino group,process for their preparation, and their use.

Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.

Abstract: A process for production of l-alkylthiomethanediphosphonic acid compound or 1-arylthiomethanediphosphonic acid compound characterized by removing a thiolate byproduct as an insoluble salt, in the condensation represented by the following formula: ##STR1## wherein R'.sub.1 represents a linear or branched alkyl group having 1 to 6 carbon atoms, R.sub.2 represents an alkyl or aryl group, R.sub.1 represents a pharmaceutically allowable cation, hydrogen atom, or linear or branched alkyl group having 1 to 6 carbon atoms. The present invention significantly improves the yield compared with conventional methods, and simplifies the purification process at the same time, thus is extremely useful in an economical and industrial points of view.

Abstract: An object of the present invention is to provide a safe method of commercially producing optically active aminoalcohol derivatives, which serve as intermediates for the synthesis of medicinal chemicals such as the immunopotentiating anticancer agent bestatin, in a simple and easy manner in high yields and with high levels of selectivity.The present invention consists in a method of producing 3-amino-1-nitro-4-phenyl-2-butanol derivatives of the general formula (1) ##STR1## wherein R.sup.1 and R.sup.2 each independently represents a hydrogen atom or an amino group protecting group, and a method of producing 3-amino-2-hydroxy-4-phenylbutyric acid derivatives derivable therefrom.