Abstract: Trifluoromethylbiphenylyl-dihalophenylazolines of formula I wherein X and Y are, independently fluorine or chlorine, and Z is O or S, their tautomers and salts are disclosed which are useful as pesticides. Compositions of these compounds of these compounds, their use in pesticidal applications, methods of manufacture thereof and intermediates in the manufacturing process are also disclosed.

Abstract: The present invention relates to novel biphenyloxazolines of the formula (I) in which X1, X2, X3, R1, R2 and R3 are each as defined in the description, to processes for their preparation and to the use of the biphenyloxazolines for controlling animal pests.

Abstract: The present invention provides an efficient synthetic strategy for the preparation of analogs that incorporate important structural elements of the marine natural product curacin A, the compositions and various uses of the compositions. The most active of these compounds at nanomolar concentrations inhibit tubulin polymerization, show growth inhibition activity, inhibited colchicines binding to tubulin and block mitotic progression. The compounds of the present invention represent some of the most potent synthetic curacin A analogs synthesized, with an activity profile rivaling that of the natural product despite the simplified structure, greater water solubility, and increased chemical stability.

Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.

Abstract: The invention concerns new vitamin D derivatives of general formula (I) a process for their production, their use for production of medicaments, and intermediate products used in the process.

Abstract: Described are a compound of formula (I), wherein X and Y are, independently of one another, florine or chlorine, and Z is O or S; and where appropriate their possible tautomers, in each case either in free form or in the form of a salt; a method for the preparation and application of these compounds and their tautomers, pesticides whose active ingredient is selected from these comounds and their tautomers; and a method for the preparation and application of these compositions, intermediates, in free form or in the form of a salt, for the preparation of these compounds and where appropriate their tautomers in free form or in the form of a salt.

Abstract: The present invention relates to new intermediates for the semisynthesis of taxanes and their preparation processes. It relates to derivatives of oxazolidines or oxazolidinones, as well as to new derivatives of baccatine III. The general process for the synthesis of taxanes according to the invention enables to obtain a product such as PACLITAXEL in only five steps from products available in the market, compared to nine steps in general, for processes of the prior art.

Abstract: Compounds having Formula I are useful for treating cancer. Also disclosed are pharmaceutical compositions comprising compounds of Formula I, and methods of treating cancer in a mammal.

Abstract: A 1,2-dioxetane derivative represented by the general formula: wherein R1, R2, R3, R4, R5, R6 and R7 each independently represents hydrogen atom, an alkyl group, or an aryl group, or one or more than one pair of R2 and R3, R4 and R5, and R6 and R7 can together form a cyclic alkyl group. The compound is easily handled because the compound itself is very stable, and it is capable of emitting light with a very high efficiency.

Abstract: New pesticidal substituted biphenytoxazolines of the formula (I) in which A, B, X, m and n have the meanings stated in the description, and new intermediates therefor.

Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.

Abstract: This invention provides a process for the preparation of a 5-methylene-1,3-oxazoline from an alkyl ketone by reacting the alkyl ketone with an acetylating agent and an acid catalyst in an appropriate solvent and at an appropriate temperature. The resulting 5-methylene-1,3-oxazoline can be chlorinated and subsequently hydrolyzed to form an .alpha.-chloroketone which is useful as a fungicide.

Abstract: This invention relates to a process for preparing perylene pigment compositions by reaction of(a) a perylene tetracarboxylic compound;(b) about 0.01 to about 20% by weight, relative to the perylene tetracarboxylic compound, of a non-pigmentary cyclic anhydride or imide of formula (I) ##STR1## wherein W is O or NR' (where R.sup.1 is hydrogen, a metal, or optionally substituted alkyl, cycloalkyl, aralkyl, or aryl), R.sup.2, R.sup.3, and R.sup.4 are various combinations of substituents and/or fused-on rings, and the dotted line is an optional double bond representing R.sup.2 --C.dbd.C--R.sup.3 ;(c) ammonia or a primary alkyl, aralkyl, or aryl amine; optionally in the presence of(d) a solvent and/or(e) one or more dispersants.

Abstract: The present invention relates to a process for the preparation of an oxazoline compound which is easily chemically converted to a beta-amino-alpha-hydroxy acid or a gamma-amino-beta-hydroxy acid. The method comprises producing a compound of the following formula (4) using .alpha.-amino acid. The produced compound (4) is subjected to an intramolecular cyclization to produce an oxazoline compound of the following formula (3). The oxazoline compound (3) is oxidized at a vinyl group with RuCl.sub.3 or NaIO.sub.4 to produce an oxazoline compound of the following formula (1) which is easily chemically converted to a beta-amino-alpha-hydroxy acid. Alternatively, the oxazoline compound (3) may also be treated with 9-borabiclo[3.3.1]nonane such that a hydroxy group is introduced into the end of the vinyl group of the oxazoline compound(3). The introduced end hydroxy group is oxidized with RuCl.sub.3 or NaIO.sub.

Abstract: Compounds of Formula I, and their agriculturally-suitable salts, are disclosed which are useful as arthropodicides ##STR1## wherein R.sup.1 -R.sup.5 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling arthropods which involves contacting the arthropods or their environment with an effective amount of a compound of Formula I.

Abstract: A method for the preparation of .beta.-amino acid compounds is provided. The method includes contacting an amine nucleophile with an .alpha.,.beta.-unsaturated amide compound in the presence of a chiral Lewis acid complex. The chiral Lewis acid complex is formed from an azophilic metal salt and a chiral bisoxazolinylmethane compound. The selective amidolysis of one enantiomer of the .beta.-aminoamide product is also described.

Abstract: The invention relates to novel diphenyloxazoline derivatives of the formula (I) ##STR1## in which a) A represents tri- to pentasubstituted phenyl andB represents substituted phenyl orb) A represents mono- or disubstituted phenyl andB represents at least trisubstituted phenyl, but where at least one substituent is not fluorine, chlorine, bromine, C.sub.1 -C.sub.6 -alkyl or -alkoxy,to a number of processes for their preparation and to their use as pest control agents.

Abstract: The invention relates to new phenylthio-oxazoline derivatives of the formula (I) ##STR1## in which A represents optionally substituted phenyl;B represents optionally substituted phenyl;D represents hydrogen or alkyl; andn represents 0, 1 or 2;to a plurality of processes for their preparation, and to their use as pesticides.

Abstract: The present invention relates to novel 4-cyclohexylphenyl-oxazolines of the formula (I) ##STR1## in which X.sup.1, X.sup.2, X.sup.3, R.sup.1 and R.sup.2 are each as defined in the description,to processes for their preparation and to their use for controlling animal pests.

Abstract: The invention relates to novel substituted oxazolines of the formula (I) ##STR1## in which A, B, D, E and G have the meaning given in the description,to a number of processes for their preparation and to their use as agents for combating pests.

Abstract: Cyclic amides of Formula (I) which are useful as fungicides wherein: A is O; S; N; NR.sup.5 ;or CR.sup.14--, G is C or N; W is O or S; X is OR.sup.1, S(O).sub.m R.sup.1 or halogen; R.sup.1, R.sup.2, and R.sup.5 are independently, in part, C.sub.1 -C.sub.6 alkyl; Y is, in part, --O--; --S(O).sub.n --,--CHR.sup.6 O--; or --CHR.sup.6 O--N.dbd.C(R.sup.7)--; Z is, in part, optionally substituted cycloalkyl, phenyl, pyridinyl, pyrimidinyl, or naphthyl; and R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.14, m, and n are defined in the disclosure, are disclosed.

Abstract: This invention relates to a process for the preparation of an .alpha.-chloroketone compound comprising the steps of(i) cyclizing an alkynyl amide to form a 5-methyleneoxazoline ##STR1## (ii) chlorinating the 5-methyleneoxazoline using trichloroisocyanuric acid to produce a chlorinated oxazoline intermediate ##STR2## and (iii) hydrolyzing the chlorinated oxazoline intermediate with an aqueous acid to produce the desired monochloroketone ##STR3## wherein Z is alkyl or substituted alkyl, aryl or substituted aryl, heteroaryl or substituted heteroaryl or phenylene,R is a hydrogen atom or alkyl, andR.sup.1 and R.sup.2 are each independently an alkyl or substituted alkyl group, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a cyclic structure.Additionally, when R is a hydrogen atom, a dichloroketone can be conveniently formed through adjustment of reaction conditions.

Abstract: Compounds represented by general formula (I) and salts thereof useful as non-tolerance-inducing antiviral agents, wherein A is O, CH.sub.2 or S; R.sup.1 is lower alkoxycarbonyl, or the like; R.sup.2 is H, OR.sup.6, F, Cl, Br, CN, NHR.sup.6 or SR.sup.6 (wherein R is H, C.sub.1 -C.sub.6 lower alkyl and the like; one of R.sup.3 and R.sup.3' is H and the other thereof is H, CN, anitrogenous group such as amino or the like; R.sup.4 is NHR.sup.6 or N.dbd.CHR.sup.6 ; and R.sup.5 is CH.sub.2 CH.sub.2 XR.sup.6 or CH(XR.sup.6)CH.sub.2 XR.sup.6 (wherein X is O, S or NH.

Abstract: This invention relates to a process for the preparation of an .alpha.-chloroketone compound comprising the steps of(i) cyclizing an alkynyl amide to form a 5-methyleneoxazoline ##STR1## (ii) chlorinating the 5-methyleneoxazoline using trichloroisocyanuric acid to produce a chlorinated oxazoline intermediate ##STR2## and (iii) hydrolyzing the chlorinated oxazoline intermediate with an aqueous acid to produce the desired monochloroketone ##STR3## wherein Z is alkyl or substituted alkyl, aryl or substituted aryl, heteroaryl or substituted heteroaryl or phenylene,R is a hydrogen atom or alkyl, andR.sup.1 and R.sup.2 are each independently an alkyl or substituted alkyl group, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a cyclic structure.Additionally, when R is a hydrogen atom, a dichloroketone can be conveniently formed through adjustment of reaction conditions.

Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

Abstract: HIV protease inhibitors inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds can be prepared by the novel methods of the present invention using the novel inventive intermediates.

Abstract: A compound represented by formula I: ##STR1## is disclosed. The compounds are active primarily against gram negative organisms. Pharmaceutical compositions and methods of treatment are also disclosed.

Abstract: Compounds of general formula I and their salts and solvates are antifungal agents and as such are useful in the treatment of various fungal infections. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.

Abstract: The present invention relates to processes for the enantioselective synthesis of hydroxypyrrolidines from amino acids. An amino methyl ester is used as the starting material. The ester is reacted with a benziminoethyl ether to produce an oxazoline or thiazoline. Specifically, L-serine methyl ester is used to produce 4-(carbomethoxy)-2-phenyl-.increment..sup.2 -oxazoline, and cysteine is used to produce the corresponding thiazoline. The oxazoline (or thiazoline) can be reduced to an aldehyde by treatment with a slight excess of DIBAL-H. The oxazoline is quenched with alcohol and reacted with (carbomethoxymethylene)triphenylphosphorane, to produce (S)-(+)-methyl (E)- and (S)-(-)-methyl (Z)-3-(4,5-dihydro-2-phenyl-4-oxazolyl)-2-propenoate. The double bond is hydroxylated to yield the diol esters. The resulting diol is then treated with aqueous acid to hydrolyze the oxazoline and recyclize to produce 3,4-dihydroxy-5-hydroxymethylpyrrolidone benzoate.

Abstract: The present invention provides a process for preparing a (4S,5R)-2,4-diphenyl-5-carboxy-oxazoline derivative, which can serve as a taxol side-chain precursor, from the treatment of a (2R,3S)-alkyl trans-3-phenyl-2,3-epoxypropionate derivative with benzonitrile in the presence of a strong acid.

Abstract: A process of making taxane derivatives by reacting Baccatin III derivatives with an oxazolidine which contains a thioester substituent at the 4-position.

Abstract: Described herein are arthropodicidal compounds, compositions and use of compounds having formula (I) wherein: A is a direct bond or C.sub.1 -C.sub.3 straight or branched chain alkylene; Z is O or S; and E, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and q are as defined in the text.

Abstract: Provided are brefeldin A derivatives of the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is H and the other of R.sub.1 and R.sub.2 is a substituent group having 1 to 12 carbon atoms containing a basic nitrogen atom or a quaternary ammonium group, or a salt thereof. These derivatives exhibit good antitumor activity, and are administrable to human patients without the problems associated with brefeldin A.

Abstract: A process for preparing polycyclic aromatic compounds by cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluoroalkylsulfonates in the presence of metallic palladium as catalyst comprises adding to the reactiona) at least one water-soluble complexing ligand andb) sufficient water for the reaction mixture to form an aqueous phase.The reaction of the invention proceeds chemoselectively so that even electrophilic groups such as esters or nitriles do not have an adverse effect on the course of the reaction.The use according to the invention of a water-soluble complexing ligand in an aqueous phase enables polycyclic aromatic compounds to be prepared in very good yields and at the same time very high purity, in particular without contamination by the complexing ligands.

Abstract: Described herein are arthropodicidal compounds, compositions and use of compounds of Formula (I) wherein the substituents are defined in the disclosure ##STR1##

Abstract: Disclosed are an oxazoline compound represented by the formula (I): ##STR1## wherein R.sup.1 represents halogen, hydrogen, alkyl, alkoxy, haloalkyl, haloalkoxy, phenyl, phenoxy, benzyl, benzyloxy, pyridyloxy, pyridylmethyloxy, alkoxy-substituted alkyl, nitro, cyanomethyloxy, haloalkylsulfonyloxy, alkylsulfonyloxy, or alkylthio; R.sup.2 represents hydrogen, halogen, alkyl, haloalkyl, alkoxy, alkylthio, or haloalkoxy; R.sup.1 and R.sup.2 may be combined to form a saturated or unsaturated 6-membered ring with oxygen; R.sup.3 represents hydrogen, halogen or alkoxy; R.sup.4 represents hydrogen, alkyl, or halogen; R.sup.5 represents hydrogen, halogen, or alkyl; X.sup.1 represents halogen, alkyl, haloalkyl, or alkoxy; X.sup.2 represents halogen, hydrogen, or alkoxy; X.sup.

Abstract: Polyoxazolines having the structural formula: ##STR1## wherein R is phenylene or alkylene containing 2 to 18 carbon atoms, R.sup.2 is C.sub.1-4 alkyl and R.sub.1 is selected from the group consisting of C.sub.1-12 alkyl, vinyl, isopropylidene, pentafluoroethyl, phenyl, hydroxyphenyl which is optionally interrupted by up to 20 ethylene oxide groups, C.sub.1-2 -alkoxyphenyl which is optionally interrupted by up to 20 ethylene oxide groups and .paren open-st.CH.sub.2 CH.sub.2 --O.paren close-st..sub.r CH.sub.3 in which r ranges from 1-20, X is NH.sub.2 or OH, n ranges from 2 to 50 and m ranges from 0 to 50, wherein R.sub.1 is hydroxyphenyl optionally interrupted by up to 20 ethylene oxide groups only when X is NH.sub.2, are polymerizable to form hyperbranched polymers which have a number average molecular weight ranging from 5,000 to 150,000, a weight average molecular weight ranging from 5,500 to 5,000,000 and a polydispersity ranging from 1.

Abstract: Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is a substituted or unsubstituted alkyl; X is --O--, --S-- or --N(R.sup.8)--, where R.sup.8 is hydrogen or alkyl; R.sup.2 is substituted or unsubstituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or substituted or unsubstituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 and R.sup.5, which may be the same or different, are each --(CH.sub.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group or monocyclic or bicyclic heteroaryl and n is integer of 0 to 3; R.sup.6 is hydrogen or substituted or unsubstituted alkyl; R.sup.7 is hydrogen or substituted or unsubstituted alkyl; and the salts, solvates, hydrates and N-oxides thereof.

Abstract: A process for the preparation of side chain-fluorinated alkyloxazoles, wherein hydroxyalkyloxazoles are reacted with an .alpha.,.alpha.-difluoroalkylamine at pressures of under 2 bar, in the presence of an inert solvent boiling at above 100.degree. C. (at normal pressure), and new fluorinated alkyloxazoles.

Abstract: Replacement with fluorine of the primary hydroxy group of 1-phenyl-2-amino-1,3-propanediol compounds wherein the secondary hydroxy group and the amino group have been suitably protected.The reaction is carried out with an inorganic fluoride in a polyglycol.New oxazoline compounds particularly useful in said process.

Abstract: A process for preparing polycyclic aromatic compounds by cross-coupling aromatic boronic acids with aromatic halogen compounds or perfluoroalkylsulfonates in the presence of metallic palladium, if desired applied to a support material, as catalyst, wherein the coupling is carried out in the presence of a ligand and a base. The process of the invention allows the yield of polycyclic aromatic compounds to be significantly increased in comparison with processes not using a ligand and thus allows a yield optimum for the Pd(0)-catalyzed cross-coupling of aromatic boronic acids with aromatic halogen compounds to be achieved.

Abstract: Novel cyclic imino ether compositions containing one or more mesogenic moieties, when polymerized, result in products having improved properties.

Abstract: 2-(2,6-difluorophenyl)-4-(2-ethoxy-4-tert-butylphenyl)-2-oxazoline. This compound is useful as miticide.

Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.

Abstract: A process for for producing a (2R,3S)-cyclohexylnorstatine or a salt thereof is disclosed, which comprises the steps of: enantioselectively hydrogenating a 4-cyclohexyl-2-halogeno-3-oxobutyric acid ester in the presence of a ruthenium-phosphine complex to produce a 4-cyclohexyl-2-halogeno-(3R)-hydroxybutyric acid ester (2); epoxidizing the compound (2) in the presence of a base to produce a 4-cyclohexyl-(2S,3R)-epoxybutyric acid ester (3); reacting the compound (3) with a lower trialkylsilyl azide in the presence of a Lewis acid to produce a (3S)-azide-4-cyclohexyl-(2S)-substituted butyric acid ester (4); subjecting the compound (4) to hydrogenolysis to produce a (2S,3S)-cyclohexylnorstatine derivative (5); and inverting the configuration at the 2-position of the compound (5).

Abstract: An oxazoline derivative having the formula: ##STR1## which is useful for control of insects, mites and/or ticks. R.sub.1 is H, halo, (halo) alkyl, alkoxy alkyl, (halo) alkoxy alkyl, (halo) alkyl thio, (halo) cycloalkyl, alkylcycloalkyl, (halo) cycloalkoxy, alkylcycloalkoxy or (R.sup.5) phenyl, phenoxyl or phenylthio or (R.sup.5) pyridyl, pyridoxyl or pyridylthio, R.sub.3 is H or methyl, R.sub.4 is phenyl or mono or disubstituted phenyl.

Abstract: The present invention relates to the derivatives of the formula ##STR1## and their tautomeric forms, as well as their addition salts, and to their use in therapeutics, especially for the treatment and prevention of cardiovascular diseases and in particular for the treatment of hypertension, cardiac insufficiency and diseases of the arterial wall, especially atherosclerosis.

Abstract: A process of preparing an oxazoline or oxazine compound of the formula ##STR1## wherein X is an atom selected from the group of oxygen and sulfur, R is selected from the group consisting of C.sub.1-10 alkyl, C.sub.1-10 fluoroalkyl, aryl and substituted-aryl, and n is 2 or 3 comprising ring-closing a compound of the formula ##STR2## wherein X is an atom selected from the group of oxygen and sulfur, R is selected from the group consisting of C.sub.1-10 alkyl, C.sub.1-10 fluoroalkyl, aryl, and substituted aryl, n is 2 or 3, and Y is a bromine or chlorine atom in the presence of a basic reagent consisting essentially of a fluoride salt supported on an inorganic solid substrate is disclosed together with the compounds, 5-bromomethyl-2-phenyl-1,3-oxazoline, 5-methylene-2-phenyl-1,3-oxazine and 4,4-dimethyl-2-vinyl-1,3-oxazoline.

Abstract: A process for preparing a compound of formula (IV): ##STR1## comprising a) contacting an oxazoline compound of formula (I): ##STR2## wherein Z is as defined hereinbefore, with a reagent capable of causing an equilibrium between oxazoline compound (I) and an oxazoline compound of formula (II) described herein, and the reagent drives the equilibrium toward oxazoline compound (II) by preferential precipitation of oxazoline compound (II);b) contacting compound (II) with a fluorinating agent to give a fluorinated oxazoline compound of formula (III) described herein; andc) hydrolyzing the compound of formula (III) to formula (IV). In an alternative embodiment, the process is directed toward a process for preparing oxazoline (II) in a single step.

Abstract: An N-alkoxymethyl benzamide derivative represented by Formula (I); ##STR1## (In the formula, reference X indicates a halogen atom, references Y.sub.1 and Y.sub.2 indicate hydrogen atoms or halogen atoms, and may be identical or different, and reference R indicates a lower alkyl group.) and a manufacturing method for this N-alkoxymethyl benzamide derivative in which a substituted benzamide and an .alpha.-haloacetal are reacted. Furthermore, a manufacturing method for benzamide derivatives in which the N-alkoxymethyl benzamide derivative represented by Formula (I) above and benzene or a derivative thereof are reacted, and a benzamide derivative is produced. The N-alkoxymethyl benzamide derivative of the present invention is a novel compound, and possesses utility as an intermediate in the manufacturing of oxazoline derivatives which possess insecticidal and anti-mite activity, and as a starting material for the synthesis of various organic compounds and the like.