- Some fluorinated heterocyclic and acyclic derivatives of chlorocarbonylsulfenyl chloride
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For the first time, fluorinated oxathialones, polyfluoroalkylchlorothioformates, chlorocarbonylpolyfluoroalkylsulfenate esters, a chlorocarbonylhexafluoroisopropylidenimino sulfenate, and a 5-tri-fluoromethyl-2-oxo-1,3,4-oxathiazole were synthesized by reacting chlorocarbonylsulfenyl chloride with RfC(O)CH2C(O)R′ (Rf = CF3; R'= CF3, OC2H5), RfO-Li+ (Rf = CF3CH2, (CF3)2C=N-Li+ and CF3C(O)NH2. Perfluorosuccinic acid and mercury(II) trifluoroacetate with ClC(O)SCI gave their respective anhydrides.
- John, Earnest Obed,Shreeve, Jean'ne M.
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Read Online
- Backside activation of σ(c-c)-bonds with Cr(VI)-reagents
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The transformations of stable propellanes 3,6-dehydrohomoadamantane (1) and 1,5-dehydrobicyclo[3.3.1]nonane (2) on treatment with chromyl oxidants in different solvents were studied. Hydrocarbon 1 with CrO2Cl2 in nonpolar solvents forms 3,6-dichloro- (3) and 3-chloro-6-hydroxy- (4) homoadamantanes in the course of backside oxidative addition. to the strained C-C bond and 3-oxobicyclo[3.3.1]nonane-7-spirocyclopropane (5) as a result of the oxidative cyclobutane ring contraction. CrO2(OAc)2/Ac2O and CrO2(OCOCF3)2/(CF3CO)2O result only in oxidative addition with the formation of the mixtures of the corresponding 6-hydroxy-3-acetates (7,9) and 3,6-diacetates (6,8). In the case of 2 the only oxidative addition takes place. Possible mechanisms of the backside oxidative addition to the C-C bond are discussed.
- Fokin, Andrey A.,Gunchenko, Pavel A.,Tkachenko, Borislav A.,Butova, Ekaterina D.,Yurchenko, Alexander G.
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- METHOD OF PREPARING HALOGENATED CARBOXYLIC ANHYDRIDES
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PROBLEM TO BE SOLVED: To provide a method for producing halogenated carboxylic anhydrides wherein: improved yield and/or purity of a product can be obtained; waste and/or by-products are easily separated from the product of the method; and/or the toxicity is reduced and/or environmental damage is reduced. SOLUTION: Trifluoroacetate acid anhydrides are prepared by, for example, reacting trifluoroacetate with sulfuric acid, oleum and/or disulfate. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPO&INPIT
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Paragraph 0022
(2021/01/19)
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- REDUCTION OF CONTENT OF CARBOXYLIC ACIDS AND DERIVATIVES THEREOF IN OLEUM, DISULFURIC ACID OR CONCENTRATED SULFURIC ACID
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The present invention concerns a process for the reduction of content of carboxylic acids and derivatives thereof in oleum, disulfuric acid or concentrated sulfuric acid. The invention further concerns a process for the manufacture of carboxylic acid anhydrides comprising the process for the reduction of content of carboxylic acids and derivatives thereof from oleum, disulfuric acid or concentrated sulfuric acid.
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Page/Page column 8-9
(2018/11/22)
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- A process for preparing trifluoroacetic anhydride method
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The invention discloses a method for preparing trifluoroacetic anhydride. A dry chemical inert solvent, white solid powdery phosphorus pentoxide and an absorbent dried and activated at the temperature of 100-130 DEG C in advance are added to a dry reaction kettle, the mixture is uniformly mixed and dispersed through mechanical stirring; trifluoroacetic acid is dropped, then the mixture is heated, subjected to reflux to have a reaction for several hours and distilled under common pressure, so that front cut fraction at the temperature of 39-50 DEG C is obtained, the obtained front cut fraction is rectified through a rectifying column, and then a reagent-grade product at the temperature of 39 DEG C-40.5 DEG C is obtained; finally, rear cut fraction higher than 50 DEG C is collected, water or a phosphoric acid aqueous solution is dropped to residues containing unreacted phosphorus pentoxide solids after the reaction, and retreatment is performed after the reaction kettle is cooled. Raw materials are cheap and easy to obtain, the solvent can be recycled, the cost is low, economic benefits are high, and the operation is standard and safe.
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Paragraph 0021; 0022; 0023; 0024; 0025; 0026; 0027-0044
(2017/05/16)
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- PROCESS FOR THE PREPARATION OF HALOGENATED CARBOXYLIC ANHYDRIDES
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The present invention relates to a process for the preparation of halogenated carboxylic anhydrides, e.g. for the preparation of trifluoroacetic anhydride. The preparation is achieved by reacting a halogenated carboxylic acid, e.g. trifluoroacetic acid, with sulfuric acid, oleum and/or disulfuric acid.
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Page/Page column 4
(2015/01/06)
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- Process for the preparation of halogenated carboxylic anhydrides
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The present invention relates to a process for the preparation of halogenated carboxylic anhydrides, e.g. for the preparation of trifluoroacetic anhydride. The preparation is achieved by reacting a halogenated carboxylic acid, e.g. trifluoroacetic acid, with sulfuric acid, oleum and/or disulfuric acid.
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Page/Page column 3
(2015/01/16)
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- USE OF PEPTIDIC VASOPRESSION RECEPTOR AGONISTS
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The present invention relates to the use of novel compounds for the manufacture of a medicament for treatment of inter alia conditions associated with critical care as well as to a method for treatment of said conditions, wherein said compounds are administered. The compounds utilised are represented by the general formula (I), as further defined in the specification.
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- Product distribution in the Cl-initiated photooxidation of CF 3C(O)OCH2CF3
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The product distribution and the mechanism of the reaction of Cl atoms with 2,2,2-trifluoroethyl 2,2,2-trifluoroacetate (TFETFA; CF3C(O)OCH 2CF3) were investigated using a 1080 L environmental chamber with in situ Fourier transform infrared (FTIR) spectroscopy detection. The experiments were performed at (296±2) K and atmospheric pressure (760±10) Torr of synthetic air free of NOx. A yield of (45W3)% was obtained for the CF3C(O)OC(O)CF3 formation. CF2O and CO were produced with estimated yields of 35 and 28%, respectively. No trifluoroacetic acid (TFA; CF3C(O)OH) was observed. The yields determined are rationalized in terms of the competitive reaction channels for the fluoroalcoxy radicals formed in the H-abstraction process: (a) reaction with O2, (b) C-C, C-O, C-H decomposition, and (c) a possible a-ester rearrangement pathway. The negligible importance of the a-ester channel, to produce TFA, was explained by the reduction of the stability of the five-membered transition state of the a-ester rearrangement. Atmospheric implications, particularly regarding the fluorocarboxylic acid formation, are discussed. Copyright
- Blanco,Barnes,Teruel, Mariano A.
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scheme or table
p. 950 - 954
(2011/09/14)
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- Practical synthesis of gem-difluorides from cyclohexanone: Synthesis of gem-bistrifluoroacetates and their reactions with fluoride nucleophiles
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Formation of ketone acylals bearing trihaloacetoxy groups and their nucleophilic geminal disubstitution by fluoride ions were investigated. Cyclohexanone reacted with trifluoroacetic anhydride without catalyst to give gem-bistrifluoroacetates via a concerted bimolecular reaction. Treatment with hydrogen fluoride under mild conditions efficiently yielded the corresponding gem-difluorides. In this reaction process, trifluoroacetic acid was recovered and converted to trifluoroacetic anhydride using P2O5. Since gem-difluorides were derived from ketones, HF and P2O5, this constitutes a practical synthesis of gem-difluorides.
- Tojo, Masahiro,Fukuoka, Shinsuke,Tsukube, Hiroshi
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experimental part
p. 29 - 35
(2010/03/30)
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- MODULATORS OF ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTORS AND THERAPEUTIC USES THEREOF
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Compounds with α7 nicotinic acetylcholine receptor (α7 nAChR) agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological and psychiatric diseases.
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- NOVEL MULTIMERIC CD40 LIGANDS, METHOD FOR PREPARING SAME AND USE THEREOF FOR PREPARING DRUGS
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The invention concerns a compound of formula (I), wherein Y represents a macrocycle whereof the cycle comprises 9 to 36 atoms, and is functionalized by three amine or COOH functions; Rc represents a group of formula H—Xa—Xb—Xc—Xd—Xe—(Xf)i—, wherein i represents 0 or 1, Xn is in particular selected among lysine, arginine, ornithine residues, Xb is in particular selected among glycine, asparagine, L-proline or D-proline residues, Xc et Xd are in particular selected among tyrosine, phenylalanine or 3-nitrotyrosine residues, Xe et Xf are in particular selected among the following amino acid residues: NH2—(CH2)n—COOH, n ranging from 1 to 10 or NH2—(CH2—CH2—O)m—CH2CH2COOH, m ranging from 3 to 6, provided that one at least of the amino acid residues Xa, Xb, Xc and Xd is different from the corresponding amino acid in the sequence of the natural CD40 143Lys-Gly-Tyr-Tyr146 fragment
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- PEPTIDE SUBSTANCE STIMULATING REGENERATION OF CENTRAL NERVOUS SYSTEM NEURONS, PHARMACEUTICAL COMPOSITION ON ITS BASE, AND THE METHOD OF ITS APPLICATION
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The invention is related to the medicinal means of treatment of diseases, traumas, as well as consequences of traumas of the central nervous system, and can be also used as a means of stimulating neurons regeneration. There is proposed a peptide glutamyl-aspartyl-arginine with general formula H-GIu-Asp-Arg-OH sequence 1 [SEQ ID NO:1] capable of stimulating the regeneration of neurons. There is also proposed a pharmaceutical composition stimulating the regeneration of neurons containing peptide glutamyl-aspartyl-arginine with general formula H-GIu-Asp-Arg-OH sequence 1 [SEQ ID NO:1] as its active base, as well as a pharmaceutically acceptable carrier. There is proposed a method of stimulating the regeneration of neurons consisting in the administration to a patient of the pharmaceutical composition, containing peptide glutamyl-aspartyl-arginine with general formula H-Glu-Asp-Arg-OH sequence 1 [SEQ ID NO:1] as its active base, in the dose of 0.01-100 μg/kg of body weight at least once a day during a period necessary for attaining the therapeutic effect, such administration being performed parenterally.
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- PEPTIDE SUBSTANCE REVEALING A STRESS PROTECTIVE EFFECT, PHARMACEUTICAL COMPOSITION ON ITS BASE, AND THE METHOD OF ITS APPLICATION
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The invention is related to the medicinal means of prevention and treatment for functional or stress induced disorders, which occur as a result of extreme impacts, and may be used as a medication revealing a stress protective effect. There is proposed a peptide glutamyl-aspartyl-glycine with general formula H-Glu-Asp-Gly-OH sequence 1 [SEQ ID NO:1], revealing a stress protective effect. There is proposed a pharmaceutical composition revealing a stress protective effect, characterized in that such composition contains an effective amount of peptide glutamyl-aspartyl-glycine with general formula H-Glu-Asp-Gly-OH sequence 1 [SEQ ID NO:1] as its active base, as well as a pharmaceutically acceptable carrier. In this case such pharmaceutical composition exists in the form suitable for parenteral or intranasal administration. There is proposed a method of prevention and/or treatment for functional or stress induced disorders, which occur as a result of extreme impacts, such method consisting in the administration to a patient of a pharmaceutical composition containing an effective amount of peptide glutamyl-aspartyl-glycine with general formula H-Glu-Asp-Gly-OH sequence 1 [SEQ ID NO:1] as its active base in the dose of 0.01-100 μg/kg of body weight, at least once a day during a period necessary for attaining a therapeutic effect. In this case such administration is performed parenterally or intranasally.
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- PEPTIDE SUBSTANCE REVEALING AN IMMUNOGEROPROTECTIVE EFFECT, PHARMACEUTICAL COMPOSITION ON ITS BASE AND THE METHOD OF ITS APPLICATION
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The invention is related to the medicinal means of prevention and correction of age-related disorders of cellular and humoral immunity and may be used as a medication revealing an immunogeroprotective effect. There is proposed a peptide glutamyl-aspartyl-proline with general formula H-Glu-Asp-Pro-OH sequence 1 [SEQ ID NO:1], revealing an immunogeroprotective effect. There is proposed a pharmaceutical composition revealing an immunogeroprotective effect containing an effective amount of peptide glutamyl-aspartyl-proline with general formula H-Glu-Asp-Pro-QH sequence 1 [SEQ ID NO:1] as its active base. In this case such pharmaceutical composition exists in the form suitable for parenteral administration. There is proposed a method of prevention and/or correction of age-related disorders of cellular and humoral immunity by stimulating the processes of lymphocytes proliferation and differentiation, such method consisting in the administration to a patient of a pharmaceutical composition containing an effective amount of peptide glutamyl-aspartyl-proline with general formula: H-Glu-Asp-Pro-OH sequence 1 [SEQ ID NO:1] in the dose of 0.01-100 μg/kg of body weight as an active base at least once a day during a period necessary for attaining a therapeutic effect. In this case the pharmaceutical composition is administered parenterally.
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- LYSOBACTIN AMIDES
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The invention relates to lysobactin amides and methods for their preparation, as well as their use for manufacturing medicaments for the treatment and/or prophylaxis of diseases, in particular bacterial infectious diseases.
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- 13-substituted milbemycin derivatives, their preparation and their use against insects and other pests
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Compounds of formula (I) and salts thereof: Wherein R1 represents methyl, ethyl, isopropyl or s-butyl; and R2 represents hydrogen or alkyl. R3 represents hydrogen, optionally substituted alkanoyl, optionally substituted alkenoyl, optionally substituted alkynoyl, alkylsulfonyl, or alkoxycarbonyl, or R2 and R3 together with the nitrogen atom to which they are attached form a saturated, optionally substituted 4- to 6-membered heterocyclic ring group. The moiety -a- together with the carbon atom to which it is attached forms a 3- to 6-membered cycloalkyl group. These compounds have anthelmintic, acaricidal and insecticidal activity.
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- Kinetics of the thermal decomposition of bis(trifluoromethyl) peroxydicarbonate, CF3OC(O)OOC(O)OCF3
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Thermal decomposition of bis(trifluoromethyl) peroxydicarbonate has been studied. The mechanism of decomposition is a simple bond fission, homogeneous first-order process when the reaction is carried out in the presence of inert gases such as N2 or CO. An activation energy of 28.5 kcal mol-1 was determined for the temperature range of 50-90°C. Decomposition is accelerated by nitric oxide because of a chemical attack on the peroxide forming substances different from those formed with N2 or CO. An interpretation on the influence of the substituents in different peroxides on the O-O bond is given.
- Burgos Paci, Maximiliano A.,Argueello, Gustavo A.,Garcia, Placido,Willner, Helge
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- NOVEL SUBSTANCE LIBRARY AND SUPRAMOLECULAR COMPLEXES PRODUCED THEREWITH
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The invention relates to a substance library, a process for the production thereof, a process for the production of supramolecular complexes using said substance library, the use of said supramolecular complexes produced using the substance library, and the use of the substance library itself.
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- Peptidic procollagen C-proteinase inhibitors
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This invention relates to compounds of Formula (I) wherein R1-R7, A, Z and n are as described in the Summary of the Invention that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for their preparation.
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- Local anesthetic compounds and uses
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Novel compounds, pharmaceutical compositions and methods are disclosed for producing local anesthesia of long-duration. The compounds of this invention are multibinding compounds that comprise from 2 to 10 ligands covalently attached to a linker or linkers, each ligand being capable of binding to a ligand binding site in a voltage-gated Na+channel to modulate the biological processes/functions thereof.
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- HETEROCYCLIC AMIDE COMPOUNDS AND PHARMACEUTICAL USE OF THE SAME
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Heterocyclic amide compounds of the formula (I) STR1 wherein each symbol is as defined in the specification, pharmacologically acceptable salts thereof, pharmaceutical compositions thereof and pharmaceutical use thereof. The heterocyclic amide compounds and pharmacologically acceptable salts thereof of the present invention have superior inhibitory activity against chymase groups in mammals inclusive of human, and can be administered orally or parenterally. Therefore, they are useful as chymase inhibitors and can be effective for the prophylaxis and treatment of various diseases caused by chymase, such as those caused by angiotensin II.
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- Des-Arg9 -BK antagonists
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The present invention provides des-Arg 9 bradykinin analogs which are selective B1 receptor antagonists.
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- HIV peptides
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It is an object of the present invention to provide preparations for the treatment or prophylaxis of AIDS and systemic lupus erythematosus and related disorders. The invention is based on the discovery of the process triggered in the immune system by HIV which leads to AIDS. HIV has a specific mechanism to activate the immune system to allow it to replicate and this same immune activation leads to an autoimmune process which eventually leads to AIDS. The preparation for treatment comprises novel synthesized peptides whose amino acid sequences are derived from a human protein called ezrin and are based on the following sequence: NH 2 ThrGluLysLysArgArgGluThrValGluArgGluLysGluCOOH SEQ ID. No. 2. The mechanism of action of these peptides is that they switch off specific retrovirally induced immune responses by immunological tolerance.
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- Peptidase inhibitors
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This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
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- 2,2,2-Trifluoroethyl aryl selenides: ArSeCH2CF3 (Ar = C6H5, p-CH3C6H4) and their derivatives ArSe(O)CH2CF3 and ArSe(X)2CH2CF3 (X = Cl, Br, OOCCF3)
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The title selenides were prepared in good yield by reacting the appropriate aryl selenolate anions with 2,2,2-trifluoroethyltosylate in refluxing tetrahydrofuran.These unsymmetrical bivalent selenides can be oxidised to the corresponding compounds of tetravalent selenium, ArSe(X)2CH2CF3 (X=Cl and Br) with elemental chlorine and bromine.The latter, upon basic hydrolysis, gave the selenoxides, ArSe(O)CH2CF3.Selenoxides have also been formed by direct reaction of the selenides with hydrogen peroxide.Upon reaction with trifluoroacetic anhydride, these gave trifluoroacetate derivatives, ArSe(OOCCF3)2CH2CF3, in quantitative yield.The compounds have been characterized via elemental analysis, infrared spectra, 1H and 19F NMR spectra, and mass spectra.
- Khajuria, R.,Bhasin, K. K.,Verma, R. D.
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- METHOD OF TREATING DISORDERS OF THE DOPAMINERGIC SYSTEMS USING 2,5-DIAMINOTETRALINES
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The invention relates to novel 2,5-diaminotetralines of the formula: STR1 wherein R1, R2, R3 and R4 are defined herein, processes for preparing them and their use in pharmaceutical compositions. The novel 2, 5-diaminotetralines are useful in treating diseases caused by disorders of the dopaminergic systems.
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- UNUSUAL REACTION CHEMISTRY IN THERMAL DECOMPOSITION OF ALKALI METAL 2-ALKOXY-2,3,3,3-TETRAFLUOROPROPIONATE SALTS
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Pyrolyses of several salts ROCF(CF3)CO2(-)M(+) (R=Me, Et, CF3CH2; M=Na, K, Cs) have been studied.The reaction chemistry shows highly unusual dependence on the nature of the alkoxy substituent and the metal cation.Product distribution are described along with some proposed mechanisms.
- Pellerite, Mark J.
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- Substituted thiazoles and oxazoles and 2-hydroxy-morpholines
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Substituted thiazoles, oxazoles and 2-hydroxy morpholine compounds useful in the treatment of diabetes mellitus and obesity are described.
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- Reactions of the Readily Accessible Electrophile, Trifluoroacetyl Triflate: A Very Reactive Agent for Trifluoroacetylations at Oxygen, Nitrogen, Carbon, or Halogen Centers
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Trifluoroacetyl triflate (TFAT) is readily prepared in 82percent yield by the dehydration (phosphorus pentoxide) of a 2:1 mixture of trifluoroacetic acid and trifluoromethanesulfonic (triflic) acid.Reactions of this highly electrophilic trifluoroacetylating reagent with alcohols, ketones, ethers, amines, and pyridines give esters, enol esters, ether cleavage, amides, and acylpyridinium ions, respectively.Reactions with ionic or easily ionizable alkyl halides give the very volatile trifluoroacetyl halides and the ionic triflate.Triphenylmethyl chloride, for example, is quantitatively converted to triphenylcarbenium triflate in a very convenient synthetic procedure.Trifluoroacetyl triflate is used in the synthesis of the first member of a new class of pyrylium salts, 2,6-dimethoxypyrylium triflate.
- Forbus, T. R.,Taylor, S. L.,Martin, J. C.
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p. 4156 - 4159
(2007/10/02)
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- Tellurium-nitrogen compounds
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With H2N-TeF5 and (CH3)3SiNHTeF5 as the starting materials numerous new tellurium-nitrogen compounds have been synthesized. Almost all of them contain the >N-TeF5 group, which stabilizes many double-bonded systems such as O=C=NTeF5 and Cl4W=NTeF5. Cl2Se=NTeF5 is a rare example of a compound containing a discrete selenium-nitrogen double bond.
- Hartl, Hans,Huppmann, Peter,Lentz, Dieter,Seppelt, Konrad
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p. 2183 - 2187
(2008/10/08)
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- Functional Micellar Catalysis. Part 5. Catalysis of Activated Amide Hydrolysis by Hydroxy and Imidazole Functionalized Surfactant Systems
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The hydrolysis of N-(n-butyl)-2,4-dinitrotrifluoroacetanilide (IX), N-acetylimidazole (Xa), and N-hexanoylimidazole (Xb), in the pH range 7-8.5, is catalysed by micelles and co-micelles (with cetyltrimethylammonium bromide) of functional surfactants containing the hydroxy-group and/or the imidazole ring .The kinetic effects here observed are significantly different from those previously reported for the same micellar reagents in the hydrolysis of p-nitrophenyl alkanoates.Such differences are ascribed to a change in the rate-limiting step of the acylation of the micellar functions, assuming a common nucleophilic mode of action of the functional micelles in the cleavage of activated esters and amides.
- Fornasier, Roberto,Tonellato, Umberto
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p. 899 - 902
(2007/10/02)
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- Intramolecular Diels-Alder Additions. 1. Additions to Anthracene and Acridine
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Intramolecular Diels-Alder reaction of suitably 9-substituted anthracenes at temperatures ranging from 25 to 220 deg C yields a wide variety of 9,12-bridged ethano- and ethenoanthracenes.Adducts having tree-, four-, and five-membered bridges, many incorporating heteroatoms such as oxygen, nitrogen, and sulfur, have been prepared.The ease of cyclization decreases with increasing bridge length.Neither the diene nor the dienophile need to carry activating groups; vinyl and ethynyl dienophiles add with equal ease.Cyclization of N-methyl-N-propargyl-9-acridinecarboxamide gives 31, the first thermal adduct of an acridine.
- Ciganek, Engelbert
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p. 1497 - 1505
(2007/10/02)
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- Non-specific tritiation of some carcinogenic aromatic amines
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2-Aminofluorene, 4-amino-3-methylbiphenyl, 4-amino-biphenyl and 4-amino-4'-fluorobiphenyl were tritiated by acid catalyzed exchange of the corresponding nitro compounds followed by catalytic reduction. The exchange reactions were carried out by heating the nitro compounds in [3H]-trifluoroacetic acid with a catalytic amount of trifluoromethanesulphonic acid (TFMS). No loss of tritium could be detected during the conversion of the tritiated nitro compounds into the corresponding amines by catalytic hydrogenation. Incorporation into the ortho position is very low (4%). During the metabolic activation and binding of the tritiated N-acetyl-2-aminofluorene to rat liver DNA in vivo, no tritium exchange occurred.
- Breeman,Kaspersen,Westra
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p. 741 - 750,748,749
(2007/10/05)
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