Abstract: The present invention pertains generally to the field of imaging compounds, and more specifically to certain 2,2-dialkyl radionuclide-labelled carboxylic acids suitable for PEWT, SPECT and/or DNP imaging. Also described are uses of such compounds in the imaging of, inter alia, cancer tumors, metastasis, Alzheimer's disease and multiple sclerosis.

Abstract: What is described are the compounds and the synthesis of [F-18]-labelled L-glutamic acid, [F-18]-labelled L-glutamate, their derivatives of the formula (I) and their use.

Abstract: There is provided a process for producing an amide compound having an excellent harmful arthropod-controlling activity and represented by the formula (3): wherein R1, R2 and R3 independently represent a C1-C6 alkyl group optionally substituted with at least one halogen atom etc., R4, R5, R6 and R7 independently represent a halogen atom etc.

Abstract: This invention is directed to a process for the preparation of high yield alkyl or aryl iodide from its corresponding carboxylic acid using N-iodo amides.

Abstract: This invention relates to homoglutamic acid derivatives suitable for labeling or already labeled with 18F or 19F, methods of preparing such compounds, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging.

Abstract: Provided is a pattern forming method comprising (i) a step of forming a film from an actinic ray-sensitive or radiation-sensitive resin composition, (ii) a step of exposing the film, and (iii) a step of developing the exposed film by using an organic solvent-containing developer, wherein the actinic ray-sensitive or radiation-sensitive resin composition comprises (A) a resin capable of decreasing the solubility for an organic solvent-containing developer by the action of an acid, (B) a compound capable of generating an acid upon irradiation with an actinic ray or radiation, (D) a solvent, and (G) a compound having at least either one of a fluorine atom and a silicon atom and having basicity or being capable of increasing the basicity by the action of an acid.

Abstract: A medical adhesive comprises a hydrophilic urethane prepolymer (UP) obtained by reacting a fluorine-containing nonaromatic polyisocyanate component (A) and a polyol component (B) having a hydrophilic polyol (B1), and a phenolic radical scavenger (PRS). The content of (PRS) is preferably 0.01 to 3% by weight based on the weight of (UP). The content of oxyethylene groups in (B) is preferably 30 to 100% by weight based on the weight of the oxyalkylene groups in (B). Preferably, (B) is a mixture of a random copolymer obtained by addition of ethylene oxide and propylene oxide to diols and polypropylene glycol. The content of isocyanate groups in the medical adhesive is 1 to 10% by weight based on the weight of (UP). The medical adhesive is suitable for bonding body tissues, such as lung, artery and heart in particular.

Abstract: Fluoroalkyl alkyl carbonates and fluorosubstituted carbamates which are suitable as additives or solvents in lithium ion batteries are prepared from fluoroalkyl fluoroformates and the respective alcohol or amine. Methanol is the preferred alcohol, dimethylamine and diethylamine are preferred amines. Fluoromethyl methyl carbonate is the preferred compound to be produced. Fluoroalkyl fluoroformates can be prepared from aldehydes and carbonyl fluoride.

Abstract: The compound of formula (8), in racemic or single enantiomeric form, is useful in making N-(diphenylmethyl)-piperazines such as cetirizine and levocetrizine. wherein Z is preferably phenyl.

Abstract: The present invention relates to a new process for the synthesis of alkyl phosphinic acids, and more particularly to a coupling reaction between an alkylhalide and a hypophosphorous acid derivative in the presence of an amine and an amineoxide.

Abstract: The present invention is to provide a safe process for the production of tert-butyl N-(2-bromoethyl)carbamate where operation is simple, handling of the final product is easy, working efficiency is good and yield is high. A process for the production of tert-butyl N-(2-bromoethyl)carbamate, characterized in that, 2-bromoethylamine or a salt thereof is made to react with an agent for introducing a tert-butoxy carbonyl group in a water-soluble solvent in the presence of sodium hydroxide and then water as a crystallizing solvent and seed crystals are added to the reaction solution whereby crystals of tert-butyl N-(2-bromoethyl)carbamate are separated out therefrom.

Abstract: The invention relates to novel triazolopyrimidines of the formula in which R1, R2, R3 and X have the meanings given in the disclosure, and acid addition salts thereof, to a plurality of processes for preparing these novel substances, and to their use for controlling unwanted microorganisms. The invention further relates to novel amines and carbamates of the formulae indicated in the description and to processes for preparing these intermediates.

Abstract: The present invention concerns prodrugs whose aromatic oxidation, particularly their enzymatic aromatic hydroxylation, results in their activation by the release of a drug moiety. It particularly concerns anti-tumor prodrugs and those which are specifically activated by the hydroxylation activity of the P-450 enzyme CYP1B1. Also provided are methods of detection of aromatic oxidation activity.

Abstract: Provided is a compound having one or more structures of the formula: 1

Abstract: A process for producing &agr;-amino-dihalogenated methyl ketone derivatives by reacting an N-protected &agr;-amino acid ester with a dihalomethyl lithium is provided. This process is suitable for the production on an industrial scale and by this process, &agr;-amino-dihalogenated methyl ketone derivatives and &bgr;-amino-&agr;-hydroxycarboxylic acid derivatives can be obtained efficiently and economically advantageously.

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: The present invention relates to a process for forming an N-&agr;-amino protected amino acid fluoride in situ by reacting an N-&agr;-amino protected amino acid with an ionic fluoride salt in the presence of a peptide coupling agent. It is also directed to the use of the amino acid fluoride thus formed in peptide synthesis.

Abstract: Per(poly)fluorinated polyoxyethylated carbamates of general formula (I) in which R.sub.F represents a perfluorinated group containing between 1 and 18 carbon atoms, W represents an oxo group or nothing, n is an integer from 1 to 10, m is from values 2 to 6, 80 or not defined, R is an alkyl group, R.sub.F W(CH.sub.2).sub.n+1 NHC(O)-- in which R.sub.F and W are as defined above, --(CHCH.sub.3 CH.sub.2 O).sub.30 (CH.sub.2 CH.sub.2).sub.80 C(O)NH(CH.sub.2).sub.n+1 R.sub.F in which R.sub.F is a perfluorinated group containing from 1 to 18 carbon atoms, R' is a hydrogen atom, an alkyl group containing between 1 and 18 carbon atoms which is optionally substituted, an optionally substituted aryl or aralkyl group, an allyl, methallyl or propargyl group or a perfluorinated chain having between 1 and 18 carbon atoms.

Abstract: The present invention is directed to a process for forming a peptide bond between a first amino acid having a free amino group and a protected carboxy group and a second amino acid or between a peptide having a free amino group and a blocking carboxy group with a second amino acid which comprises (a) reacting the second amino acid of the formula: ##STR1## with a fluoroformamidinium salt of the formula: ##STR2## and (b) reacting the product of (a) with the first amino acid or peptide.

Abstract: An object of the present invention is to provide a process for producing a .beta.-amino-.alpha.-hydroxy acid derivative via efficient and industrially utilizable steps.The present invention provides a process for producing a .beta.-amino-.alpha.-hydroxy acid derivative represented by the general formula (2) given below which comprises hydrolyzing an .alpha.-amino-.alpha.', .alpha.'-dihaloketone derivative of the general formula (1) given below in the presence of a base, followed by protecting the amino group or without protecting the same.

Abstract: The present invention is directed to the process of preparing a peptide comprising reacting a first amino acid or peptide with an amino acid fluoride of the formula: ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting groupAA is an amino acid residue andX is H or a protecting group useful,and the first amino and peptide have a free amino group and a blocked carboxy end.

Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.

Abstract: The present invention is directed to the process of preparing a peptide comprising reacting a first amino acid or peptide with an amino acid fluoride of the formula: ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting groupAA is an amino acid residue andX is H or a protecting group useful,and the first amino and peptide have a free amino group and a blocked carboxy end.

Abstract: The present invention relates to novel .alpha..sub.1 -adrenoceptor antagonists of Formula I: ##STR1## in which: p is 0 or 1;t is 0, 1 or 2;X is O, S or NR.sup.6 (in which R.sup.6 is hydro or (C.sub.1-6)alkyl);Y and Z are independently CH or N;R.sup.1 is hydro, hydroxy, halo, nitro, amino, cyano, (C.sub.1-4)alkylthio, acetylamino, trifluoroacetylamino, methylsulfonylamino, (C.sub.1-6)alkyl, (C.sub.3-6)cycloalkyl, (C.sub.3-6)cycloalkyl (C.sub.1-4)alkyl, oxazol-2-yl, aryl, heteroaryl, aryl (C.sub.1-4)alkyl, heteroaryl (C.sub.1-4)alkyl, (C.sub.1-6)alkyloxy, (C.sub.3-6)cycloalkyloxy, (C.sub.3-6)cycloalkyl (C.sub.1-4)alkyloxy, 2-propynyloxy, aryloxy, heteroaryloxy, aryl (C.sub.1-4)alkyloxy or heteroaryl (C.sub.1-4)alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms and aryl or heteroaryl is optionally substituted with one to two substituents independently selected from halo and cyano);R.sup.2 is hydro, hydroxy, halo, cyano, (C.sub.1-6)alkyl or (C.sub.

Abstract: The invention relates to a new process for the preparation of substituted diaminodicarboxylic acid derivatives of the formula ##STR1## in a high yield by a modified Kolbe synthesis.

Abstract: A process for the manufacture of N-protected .alpha.-aminoketones and N-protected .alpha.-aminoalcohols of the formula ##STR1## wherein X is halogen, one of Q.sup.1 and Q.sup.2 is hydrogen and the other is hydroxy or Q.sup.1 and Q.sup.2 together are oxo, R.sup.1 is an amino protecting group and R.sup.2 is hydrogen or the characterizing group of an .alpha.-aminocarboxylic acid,starting from the corresponding lower alkyl N-protected .alpha.-aminocarboxylates via corresponding lower alkyl N-silyl protected .alpha.-aminocarboxylates.

Abstract: This invention relates to perfluoroalkyl group terminated urethanes, thiourethanes and ureas of the general formula(R--X--CONH).sub.m Awhere m is 1, 2 or 3, R is R.sub.f -E and optionally R.sub.1 with the proviso that at least one R is R.sub.f -E, R.sub.f is a perfluoroalkyl group, R.sub.1 is a hydrocarbon group, E is a divalent linking group, X is --O--, --S--, --NR.sub.2 -- and R.sub.2 is H or lower alkyl and A is R.sub.f E or R.sub.1 if m is 1 and a divalent or trivalent linking group if m is 2 or 3 respectively.Compounds of this general formula are useful as solid lubricants or as additives for waxes and resins providing lubricating properties.

Abstract: Normally liquid, omega-hydrofluoroalkyl ether compounds (and selected mixtures thereof) have a saturated perfluoroaliphatic chain of carbon atoms interrupted by one or more ether oxygen atoms. The compounds can be prepared, e.g., by decarboxylation of the corresponding fluoroalkyl ether carboxylic acids and are useful, e.g., in cleaning and drying applications.

Abstract: Process for the preparation of phosphorus-containing L-amino acids, their derivatives and intermediates for this processL-amino acids of the formula I and salts thereof, ##STR1## in which R.sup.1 to R.sup.5 are defined as in claim 1 and n is 0 or 1, are obtained according to the invention bya) reacting an optically active S-homoserine lactone of the formula II, ##STR2## with hydrogen chloride in the presence of an alcohol of the formula R.sup.5 --OH to give novel compounds of the formula III, ##STR3## in which R.sup.3, R.sup.4 and R.sup.5 are defined as in formula I, except that R.sup.5 =H, andb) reacting the resulting compound of formula III with a compound of formula IV,R.sup.1 (O).sub.n -R(OR.sup.2).sub.2 (IV)and if desired, hydrolyzing the product to give a compound of formula I, in which R.sup.5 =H.

Abstract: A compound of the formula ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting group or hydrogenAA is an amino acid residue andX is H or a protecting group useful as a coupling agent in peptide synthesis.

Abstract: The asymmetric hydrogenation of aliphatic .alpha.-keto esters in the presence of rhodium catalysts which contain as chiral ligand a diphosphine of formula IV(R.sub.3).sub.2 P--Q--P(R.sub.3)hd 2 (IV)wherein R.sub.3 is phenyl, C.sub.1 -C.sub.6 alkylphenyl or C.sub.1 -C.sub.6 alkoxyphenyl, and Q is [2,2,1]-bicyloheptan-1,2-ylene or [2,2,1]-bicyclohept-4,5-en-1,2-ylene, gives the corresponding (R)- or(S)-.alpha.-hydroxycarboxylic acid esters in high rates of chemical conversion and in high enantiomer excesses.

Abstract: Processes for producing carbamates comprise contacting a first reactant selected from primary amine components, secondary amine components, urea components and mixtures thereof; carbon monoxide; at least one organic hydroxyl component and at least one oxygen-containing oxidizing agent in the presence of a catalyst composition comprising at least one metal macrocyclic complex, preferably in the further presence of a halogen component.

Abstract: HMG-CoA reductase inhibitors of formulae (I) and (II) are disclosed.

Abstract: Substituted 1-alkyl carbamates of the formula ##STR1## in which: R is a member selected from the group consisting of halogen, trifluoromethyl, cyano, NO.sub.2 and C.sub.1 -C.sub.3 haloalkyloxy;R.sub.1 is selected from the group consisting of C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 haloalkyl; andR.sub.2 is selected from the group consisting of H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkoxyalkyl, C.sub.1 -C.sub.4 haloalkyl and C.sub.1 -C.sub.4 alkenyl;and their use as herbicides is disclosed herein.

Abstract: Substituted phenoxy, phenylthio and anilino compounds, intermediates therefor, synthesis thereof, and their use for the control of pests.

Abstract: A process for preparing a perfluoroalkyl-substituted compound is disclosed. The process comprises reacting a halopolyfluoroalkane having 1 to 20 carbon atoms with a compound selected from the group consisting of (1) a substituted or unsubstituted ethylene, (2) a substituted or unsubstituted acetylene and (3) a substituted or unsubstituted allylsilane, in the presence of a metal-carbonyl complex of the metal of the Group VIII of the Periodic Table. Alternatively, the reaction between the halopolyfluoroalkane and the substituted or unsubstituted allylsilane is effected under radical generating condition.

Abstract: Poly(alkylene carbonate) monoahls and polyahls useful as nonionic surfactants and having a poly(alkylene carbonate) backbone are prepared by reacting an oligomeric poly(alkylene carbonate) polyahl with a compound having mono- or difunctional active hydrogen moieties, such as alcohols, carboxylic acids, mercaptans, amides, primary or secondary amines, or substituted phenols, optionally in the presence of a catalyst, under transesterification conditions.

Abstract: Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.

Abstract: An improved for preparing N-substituted carbamate comprising reaction of a selected olefin or alcohol with a carbamate in the presence of a catalyst comprising a blend of a perfluorinated sulfonic acid polymer and a perfluorinated polymer diluent in a substantially nonpolar reaction mixture.

Abstract: Alkyl esters of 2-fluoro-1-methoxyethylcarbamic acid, which are useful intermediates in the preparation of compounds, such as 4-amino-5- fluoropentanoic acid, are prepared by the electrochemical anodic oxidation of esters of 2-fluoroethylcarbamic acid in the presence of methanol and an electrolyte.

Abstract: Novel 2,2-dihalovinyl haloformates are described of general formula: ##STR1## in which: X is a chlorine or bromine atom;X.sub.1 and X.sub.2 are the same or different and are chlorine or bromine.The compounds are prepared by reaction of a 1,2,2,2-tetrahaloethyl haloformate of formula: ##STR2## in which: X.sub.1, X.sub.2 and X are as described hereinabove;X.sub.3 is chlorine or bromine and is always bromine when X.sub.1 and/or X.sub.2 is bromine andX.sub.4 is chlorine or bromine, with a metal such as zinc or magnesium in a solvent.The novel compounds are very useful for the preparation of 2,2-dihalovinyl carbonates and carbamates which may be used as insecticides or as comonomers.

Abstract: A process for the preparation of vinyl carbamates of formula I ##STR1## is described which comprises heating an .alpha.-halogeno-carbamate of formula II ##STR2## in which X is a halogen atom at a temperature between 70.degree. and 250.degree. C. for a period of time between several minutes up to several hours. R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are the same or different. The process is applicable to a great variety of products in which R.sub.1, R.sub.2, R.sub.3, and R.sub.4 have different meanings. The process permits to prepare in a simple and economical fashion, vinyl carbamates, which have industrial value and novel vinyl carbamates.

Abstract: This invention relates to novel (acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs having a primary or secondary amine function thereon. Hydrolytic enzymes are used to trigger the regeneration of the parent amine drug of the carbamate prodrug moiety. The case also contains pharmaceutical composition, method of treatment and process claims.

Abstract: Surfactants which are blocked against surfactant action (identified herein as "photolabile blocked surfactants") by a photolabile protective or masking group but which, on exposure to actinic radiation, become unblocked are provided. Coating compositions in which surfactant is formed on irradiation are provided by blending the photolabile blocked surfactant with polymeric film-forming materials.Compositions containing the photolabile blocked surfactants are useful when employed as protective coatings on various substrates or as the adhesive in a pressure sensitive adhesive tape. Although initially well adhering to a substrate, such compositions may be readily removed from the substrate following exposure of the same to suitable radiation which unblocks the surfactant to permit it to regain its surfactant activity.

Abstract: Certain novel derivatives of carbamates and their use for the control of pests.

Abstract: This invention is for .gamma.-allenyl-.gamma.-aminobutyric acid derivatives which are .gamma.-aminobutyric acid transaminase inhibitors.

Abstract: Halogenoalkylcarbamic acid esters of the formula ##STR1## in which R, R.sup.1 and R.sup.2 independently of one another represent methyl which is optionally substituted by halogen, at least one of the methyl groups R, R.sup.1 and R.sup.2 being substituted by at least one halogen atom,R.sup.3, R.sup.4 and R.sup.5 are identical or different and individually represent hydrogen or optionally substituted alkyl andn represents 0 or 1,synergize the action of known arthropodicides.

Abstract: This invention relates to a process for preparing urethanes by reacting a solution of a nitrogen-containing organic compound and a hydroxyl-containing organic compound with carbon monoxide in the presence of a ruthenium catalyst comprising a bis phosphine ligand.

Abstract: A process for the preparation of urethanes. Urethanes having the general formula R.sub.1 (NHCOOR.sub.2).sub.n are reacted with an alcohol at a temperature of 120.degree. to 400.degree. C. in amounts such that, for every mol of the urethane, at least one mol of the alcohol is present. R.sub.1 is a radical obtained by removing the isocyanate groups from an n-functional organic isocyanate, which isocyanate has a boiling point greater than 100.degree. C. at atmospheric pressure. R.sub.2 is a radical obtained by removing the hydroxyl group from a monohydric alcohol which has a boiling point greater than 140.degree. C. at atmospheric pressure.

Abstract: 2-Substituted alkyl (2-substituted alkyl)carbamates useful as intermediates in the preparation of epoxy derivatives of olefins are prepared by reacting 2-oxazolidones with an olefin and an electrophile such as halogen.