Abstract: There is disclosed a process for producing taurine from aziridine by (a) adding gaseous aziridine or a solution of aziridine to a solution of ammonium bisulfite, or ammonium sulfite, or a mixture of ammonium bisulfite and ammonium sulfite to form ammonium taurinate; (b) decomposing ammonium taurinate by heating and removing ammonia from (a) to obtain a crystalline suspension of taurine; and (c) separating taurine by means of solid-liquid separation.

Abstract: The method relates to the field of asymmetric allylic amination and comprises preparing a chiral N-substituted allylic amine compound from the corresponding allylic substrates and substituted hydroxylamines, in the presence of a catalyst, said catalyst comprising copper compounds and a chiral ligand. Examples of chiral amine compounds which can be made using the method include Vigabatrin, Ezetimibe Terbinafine, Naftifine 3-methylmorphine, Sertraline, Cinacalcet, Mefloquine hydrochloride, and Rivastigmine. There are over 20,000 known bioactive molecules with chiral N-substituted allylic amine substructure. The method may also be used to produce non-natural chiral ?-aminoacid esters, a sub-class of chiral N-substituted allylic amine compounds. Examples of ?-aminoacid ester which can be produced by the disclosed method, include, but are not limited to, N-(2-methylpent-1-en-3-yl)benzenamine and Ethyl 2-methylene-3-(phenylamino)butanoate.

Abstract: The present invention provides methods for catalyzing the conversion of an olefin to any compound containing one or more cyclopropane functional groups using heme enzymes. In certain aspects, the present invention provides a method for producing a cyclopropanation product comprising providing an olefinic substrate, a diazo reagent, and a heme enzyme; and admixing the components in a reaction for a time sufficient to produce a cyclopropanation product. In other aspects, the present invention provides heme enzymes including variants and fragments thereof that are capable of carrying out in vivo and in vitro olefin cyclopropanation reactions. Expression vectors and host cells expressing the heme enzymes are also provided by the present invention.

Abstract: Disclosed is a method for the transition metal-mediated oxidation of C—H bonds to form C—O or C—S bonds. The methods are useful for the formation of ethers (R—OR?) from alcohols, R?OH, and sp3-hybridized C—H bonds in substrates, R—H. Aryl or heteroaryl acetates may also be used for C—H to C—OAr bond formation. The methods are also useful in the preparation of C—S bonds from acetyl-protected thiols, MeC(O)SR, and disulfides, RSSR. Advantageously, the methods minimize reaction steps, the handling of oxidized intermediates, and environmental impact.

Abstract: There is provided the use as reducing agents of alpha-hydroxycarbonyl compounds capable of forming cyclic dimers. There is also provided corresponding methods of reducing reducible compounds, particularly reduction-activated prodrugs. Examples of the alpha-hydroxycarbonyl compounds used are dihydroxyacetone, glycolaldehyde, glyceraldehyde, erythrose, xylulose, erythrulose or 3-hydroxy-2-butanone.

Abstract: Use of aziridines for stabilizing iodine-containing compounds, especially biocides.

Abstract: Disclosed are metal-bound tetracarbene catalysts, such as iron based aziridination catalyst, having the formula: wherein X is a group 6, 7, 8, 9, or 10 metal and wherein Z is a hydrogen, alkyl, aryl or organic group, wherein the alkyl, aryl or organic group is optionally are independently substituted. In a specific example, a metal-bound tetracarbene catalyst has the formula: Also disclosed are methods of making (synthesizing), transmetallation reagents, these agents, metal-bound tetracarbene catalysts, and a method of catalytic alkene aziridination, using the disclosed metal-bound tetracarbene catalysts.

Abstract: A process for aziridination of olefins using NaIO4/alkali metal bromide/H+/Chloramine-T combination in presence of dipolar aprotic solvent under ambient conditions to obtain aziridines is disclosed.

Abstract: A crosslinkable, pre-adhesive composition is described comprising an acid-functional (meth)acrylate copolymer and an aziridine crosslinking agent, which when crosslinked provides a pressure-sensitive adhesive and pressure-sensitive adhesive articles.

Abstract: One aspect of the present invention relates to a method for the transition metal (e.g., Cu(I)) mediated amidation of C—H bonds using electron-rich aliphatic azides. In certain embodiments, the methods are useful for the C—H insertion of nitrenes generated and stabilized by a ?-diketiminato metal catalyst. In certain embodiments, said nitrenes are generated from organoazides, or by oxidation of the corresponding amine. Another aspect of the present invention relates to olefin aziridination using said ?-diketiminato metal catalysts. In addition, the methods of the present invention include stereoselective C—H bond aminations and olefin aziridinatons. In certain embodiments, the methods are conducted in an aerobic environment. In certain embodiments, the present invention relates to the use of O2 as an oxidant, wherein water is the byproduct of oxidation; this fact avoids the generation of toxic byproducts and renders the methods atom economical.

Abstract: Vinyl oxiranes are rearranged to 2,5-dihydrofuran using catalyst (III) or (IV). The 2,5-dihydrofuran can be reduced to tetrahydrofuran. 3,4-Epoxy-1-butene substrate is converted to 2,5-dihydrofuran which in turn is converted to tetrahydrofuran. Substrate for making 3-methyltetrahydrofuran is prepared from isoprene. Substrate for making 2-methyltetrahydrofuran is prepared from piperylene. Reactions analogous to that with vinyl oxiranes are carried out with vinyl thiiranes and vinyl aziridines.

Abstract: (R)-2-Arylpropionamide compounds of formula (I) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear leukocytes (leukocytes PMN) and of monocytes at the inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use in the inhibition of the chemotaxis of neutrophils and monocytes induced by the C5a fraction of the complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of neutrophils and monocytes and the IL-8-induced chemotaxis of PMN leukocytes.

Abstract: Use of aziridines for stabilizing iodine-containing compounds, especially biocides.

Abstract: The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention is able to reduce preparation costs by using low cost reagents on reaction and is able to be used in mass production by improving yield.

Abstract: The invention relates to compounds of the formula (I), in which X, -Q1-Q2- and RF have the meaning indicated in Claim 1, as ionic liquids, and to a process for the preparation thereof.

Abstract: Described herein is a mixture comprising: a non-self-crosslinking polymer; and a modifying compound comprising at least two different functional groups. The first functional group of the modifying compound is capable of reacting with the non-self-crosslinking polymer and the second functional group is capable of crosslinking with a curing agent. Also, described are compositions, curable polymeric compositions, articles using such curable polymeric compositions, and methods of making cured polymeric compositions.

Abstract: The invention features oligofluorinated cross-linked polymers and their use in the manufacture of articles and coating surfaces.

Abstract: A method of combating a parasitic protozoal infection of a host organism, the method comprising administering tretazicar to the host organism. Tretazicar is the compound 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB 1954), and the parasitic infection is preferably an infection of Trypanosoma cruzi, T. b. brucei, Leishmania spp. particularly L. infantum, Cryptosporidium or Giardia spp.

Abstract: A process for the preparation of a nucleophilic addition product of an aziridine and a nucleophile, the process comprising treating the arizidine with the nucleophile in the presence of a biaryl phosphoric acid catalyst.

Abstract: The invention relates to a method for producing injectable medicament preparations containing a therapeutically and/or diagnostically effective substance which is comprised of an active agent, of a spacer molecule and of at least one protein-binding molecule. After being brought into contact with the body, said therapeutically and/or diagnostically effective substance covalently bonds to the body fluid constituents or tissue constituents via the protein-binding molecule, thus providing a form of transport of the active agent that an be hydrolytically or enzymatically cleaved, according to pH, in the body while releasing the active agent.

Abstract: Process for preparing an N-unsubstituted or N-substituted aziridine of the formula which comprises reacting an olefin of the formula I where R1 to R5 are each, independently of one another, hydrogen, a linear or branched alkyl radical having from 1 to 16 carbon atoms, a hydroxyalkyl radical having from 1 to 4 carbon atoms, a cycloalkyl radical having from 5 to 7 carbon atoms, a benzyl or phenyl radical which in each case may be substituted in the o, m or p position of the phenyl radical by methoxy, hydroxy, chlorine or alkyl radicals having from 1 to 4 carbon atoms and the radical R1 or R2 together with the radical R3 or R4 may be closed to form a 5- to 12-membered ring or the radicals R1 and R2 may be closed to form a 5- to 12-membered ring, with ammonia or a primary amine of the formula R5NH2 in the presence of iodine or bromine.

Abstract: One aspect of the present invention relates to a method for the transition metal (e.g., Cu(I)) mediated amidation of C—H bonds using electron-rich aliphatic azides. In certain embodiments, the methods are useful for the C—H insertion of nitrenes generated and stabilized by a ?-diketiminato metal catalyst. In certain embodiments, said nitrenes are generated from organoazides, or by oxidation of the corresponding amine. Another aspect of the present invention relates to olefin aziridination using said ?-diketiminato metal catalysts. In addition, the methods of the present invention include stereoselective C—H bond aminations and olefin aziridinatons. In certain embodiments, the methods are conducted in an aerobic environment. In certain embodiments, the present invention relates to the use of O2 as an oxidant, wherein water is the byproduct of oxidation; this fact avoids the generation of toxic byproducts and renders the methods atom economical.

Abstract: This invention relates to compositions and methods for achieving the efficient aziridination of organic molecules, especially olefins. More specifically, the invention is directed to a mild, selective, and efficient aziridination protocol that involves catalysis by a mixed-valent dirhodium(II,III) catalyst (Rh25+). Especially preferred sources for forming such mixed-valent dirhodium(II,III) catalyst (Rh25+) are dirhodium(II) carboxamidates, such as dirhodium(II) caprolactamate, and their derivatives and analogues.

Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.

Abstract: There is provided a series of substituted oxime-containing acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

Abstract: Fungicidal compounds of the general formula (1) wherein X, Y, Z, R1, R2, R3, R4 and R5 have the definitions given in claim 1

Abstract: A sphingomyelin analog represented by the following formula wherein R1 is C1-20 alkyl group, R2 is C1-20 alkyl group, aryl group or C1-6 alkyl group substituted by aryl group, and Z is photoaffinity-labeled group, or its optically active compound.

Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.

Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.

Abstract: The invention relates to a process for reducing the monomeric aziridine content in a polyaziridine forming reaction mixture by adding to the polyaziridine forming reaction mixture an excess of an organic carbonate scavenger wherein the excess is based on the equivalent ratio of scavenger to monomeric aziridine, and to a product obtained by this process and to a coating composition containing the product obtained by the process.

Abstract: In the production of aziridines or N-vinyl amides respectively from an alkanolamine or an alkanolamide by the known method comprising a reaction step, a collecting step and/or a condensation step, a purifying step, and a recovering step, this invention is directed toward preventing formation of a solid substance in the vacuum pumps and the vacuum lines. The object of this invention is accomplished by performing the decompression at the purifying step and the decompression at the recovering step in mutually different decompression systems.

Abstract: This invention offers a photoreactive labeling reagent consisting of a novel biotinylated phenyldiazirine compound; a photoaffinity labeling reagent consisting of a saccharide-linked biotinylated phenyldiazirine compound where a saccharide compound is introduced into the novel compound; and a novel diazirine compound for such a reagent. The invention covers a biotinylated phenyldiazirine compound of the following formula (II); a phenyldiazirine compound which is an intermediate for synthesizing the above; a saccharide-linked biotinylated phenyldiazirine compound derived from the compound of the formula (II) and a saccharide compound and a method for manufacturing the same; a photoreactive labeling reagent containing the compound of the formula (II); a photoaffinity labeling reagent containing the saccharide-linked biotinylated phenyldiazirine compound; and a method for labeling a saccharide receptor using the reagent.

Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of Cathepsins K and L. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract: This invention provides biphenyl derivatives containing (i) a (biphenyl-2-yl)oxycarbonylamino- or (biphenyl-2-yl)aminocarbonylamino-substituted (2-7C)azacycloalkyl or (5-10C)azabicycloalkyl group; (ii) a substituted 2-(4-hydroxyphenyl)-2-hydroxyethylamino group; and a divalent hydrocarbon group, where each group is further defined and optionally substituted as described in the specification. The biphenyl derivatives of the invention possess both &bgr;2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract: Compounds and methods are provided for a single-pot covalent attachment of a label to nucleic acids comprising forming a covalently attachable labeling reagent for alkylating the molecule. Then, combining the covalently attachable labeling reagent with a mixture containing the molecule, under conditions wherein the labeling reagent has reactivity with the molecule thereby forming a covalent bond.

Abstract: Compounds of formula (I) 1

Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein X is selected from halogen and R5SO4 where the halogen is preferably Cl, Br or I; R, R1 and R2 are each individually selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl, or two of R, R1 and R2 together with the nitrogen atom to which they are attached form a C3 to C6 saturated or unsaturated ring optionally containing in the ring one or more additional hetero atoms selected from O, S and N atoms; R3 and R 4 are each individually selected from C1 to C6 alkyl, C1 to C6 hydroxyalkyl, C1 to C6 alkoxy, C1 to C6 aminoalkyl or R3 and R4 together form a C1 to C5 alkylene group; and R5 is selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl.

Abstract: Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.

Abstract: Amine compounds having a cyano group are useful in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.

Abstract: An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.

Abstract: In the production of aziridines or N-vinyl amides respectively from an alkanolamine or an alkanolamide by the known method comprising a reaction step, a collecting step and/or a condensation step, a purifying step, and a recovering step, this invention is directed toward preventing formation of a solid substance in the vacuum pumps and the vacuum lines. The object of this invention is accomplished by performing the decompression at the purifying step and the decompression at the recovering step in mutually different decompression systems.

Abstract: Unsaturated 1-Amino-alkylcyclohexane compounds which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borna virus, anti-HSV and anti-Hepatitis C virus activity.

Abstract: Disclosed is an efficient, inexpensive method for the preparation of chiral aziridines on a large scale.

Abstract: In order to carry out various vapor-phase reactions (e.g., the preparation of aziridine compounds by a vapor-phase intramolecular dehydration reaction) with industrial advantages, there is provided a process which can effectively prevent the adhesion of tarry matter to piping and the like. This process is applicable, for example, to the preparation of aziridine compounds by using a reactor for carrying out the vapor-phase intramolecular dehydration reaction of an alkanolamine, a collection column for collecting an aziridine compound present in the reaction gas, and a distillation column for distilling the collector liquid to obtain a purified aziridine compound, and is characterized in that at least the piping section extending from the outlet of the reactor to the inlet of the collection column is maintained at a temperature which is not lower than 200° C., or in that the reaction gas is brought into contact with a collector prior to its introduction into the collection column.

Abstract: The invention relates to compounds of the general formula (I): 1

Abstract: A compound comprising a target cell-specific portion and human NAD(P)H:quinone reductase 2 (NQO2) or a variant or fragment or fusion or derivative thereof which has substantially the same activity as NQO2 towards a given prodrug, or a polynucleotide encoding said NQO2 or said variant or fragment or fusion or derivative. A recombinant polynucleotide comprising a target cell-specific promoter operably linked to a polynucleotide encoding human NAD(P)H:quinone reductase 2 (NQO2) or a variant or fragment or fusion or derivative thereof which has substantially the same activity as NQO2 towards a given prodrug. The compounds and polynucleotides are useful in a method of treating a patient in conjunction with a suitable prodrug.

Abstract: One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

Abstract: Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.

Abstract: In order to carry out various vapor-phase reactions (e.g., the preparation of aziridine compounds by a vapor-phase intramolecular dehydration reaction) with industrial advantages, there is provided a process which can effectively prevent the adhesion of tarry matter to piping and the like. This process is applicable, for example, to the preparation of aziridine compounds by using a reactor for carrying out the vapor-phase intramolecular dehydration reaction of an alkanolamine, a collection column for collecting an aziridine compound present in the reaction gas, and a distillation column for distilling the collector liquid to obtain a purified aziridine compound, and is characterized in that at least the piping section extending from the outlet of the reactor to the inlet of the collection column is maintained at a temperature which is not lower than 200° C., or in that the reaction gas is brought into contact with a collector prior to its introduction into the collection column.

Abstract: The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.