1662results about "Sulfonic acid amide preparation" patented technology

This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: whereinR1, R2, R3, R4, R5 is independently H, halogen, C1–C4 alkyl, nitro, nitrile, C1–C4 alkoxy, halogenated C1–C4 alkyl, or halogenated C1–C4 alkoxy, wherein at least one of R1, R3, and R5 is nitro;R6 is H or protected or unprotected side chain of natural or unnatural α-amino acid; andB is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases.

The invention provides substituted diaryl compounds as shown in general formula (I) or their pharmaceutically acceptable salts, and also provides a preparation method; a class of novel broad-spectrum antiviral compounds and pharmaceutical salts targeting cytokines are screened and obtained through studies on structure-activity relationship and action mechanism of active compounds; the compounds not only have significant broad-spectrum antiviral activity, but also have the advantages of low toxicity and good pharmaceutical properties.

Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration are provided, and methods of preparation of the modified amino acid compound are provided.

The invention provides a soluble epoxide hydrolase inhibitor, which has the following structural formula I, wherein R1 is N-R2R3; R2 and R3 are hydrogen, C1-C4 alkyl, aromatic ring, aromatic heterocyclic ring, or C1-C4 alkyl connected with the aromatic ring or the aromatic heterocyclic ring respectively; and the R2 can also be connected with the R3 to form a ring, then R1 is a quinary, hexahydricor heptabasic heterocyclic ring containing 1 nitrogen atom or 1 oxygen atom, and the nitrogen atom can be directly connected with the hydrogen and can also be connected with the C1-C4 alkyl. Rat experiment group results in an anesthesia state and a non-anesthesia state show that the inhibitor has certain blood pressure reducing effect, can be used for preparing medicaments for preventing and treating cardiovascular diseases, and has broad clinical application prospect. The invention provides a preparation method.

The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-oxygen bond between the oxygen atom of an alcohol and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. The present invention also relates to copper-catalyzed methods of forming a carbon-carbon bond between a reactant comprising a nucleophilic carbon atom, e.g., an enolate or malonate anion, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. Importantly, all the methods of the present invention are relatively inexpensive to practice due to the low cost of the copper comprised by the catalysts.

The present invention provids a method for producing fluorosulfonylimides more safely, rapidly and efficiently, which enables suppression of production of by-products, and fluorosulfonylimides. The method for producing a fluorosulfonylimide salt of the present invention includes a step of reacting a fluoride compound containing at least one element selected from the group consisting of elements of Group 11 to Group 15 and Period 4 to Period 6 (excluding arsenic and antimony) with a compound represented by the following general formula (I) to give a fluorosulfonylimide salt represented by the general formula (II): [Chemical Formula 1] wherein R1 denotes at least one element selected from the group consisting of elements of Group 11 to Group 15 and Period 4 to Period 6 (excluding arsenic and antimony); R3 denotes fluorine, chlorine or a fluorinated alkyl group having 1 to 6 carbon atoms; R4 denotes fluorine or a fluorinated alkyl group having 1 to 6 carbon atoms; and m denotes an integer of 2 or 3.

The invention discloses a synthesis method of an alkali metal salt containing sulfonyl chloride or phosphorus imide: the alkali metal salt is prepared by subjecting compound (V-2) and sulfuryl chloride or phosphorus oxychloride to nucleophilic substitution under the presentation of acid binding agents; the invention further discloses a synthesis method of an alkali metal salt containing fluorine sulfonyl or phosphorus imide, the alkali metal salt is prepared by reacting (sulfonyl chloride) (perfluorinated alkyl) imide salt (V-1) or (dichloro phosphoryl) (perfluorinated alkyl sulfonyl) imide salt (V-2) with fluorinated reagents. The synthesis methods have the advantages that the experiment condition is mild, and the used materials are convenient to store and prepare; the preparation rate is high, the purification is simple, the preparation cost is low, and the methods are suitable for mass industrial preparation. The preparation rate and the purity of the resultants are high, and the resultants can be used as lithium salt electrolyte materials for lithium batteries, or for preparing catalytic agents, and for synthesizing high-performance ionic liquids.

(1) Prostaglandin (PG) E2 antagonist or agonist containing carbocyclic sulfonamides represented by the compound of the formula (I): cyclodextrin clathrates thereof, non-toxic salts thereof as active ingredient, (2) carbocyclic sulfonamides represented by the compound of the formula (II): cyclodextrin clathrates thereof, non-toxic salts thereof, (3) process for the preparation of the compound represented by the compound of the formula (II) described hereinbefore, (4) PGE2 antagonist or agonist containing the compound represented by the compound of the formula (II) as active ingredient. The compounds represented by the compounds of the formula (I) and (II) can be adapted to medicines which possess an inhibitory effect of uterine contraction, an analgetic action, an inhibitory effect of digestive peristalsis, a sleep-inducing effect as PGE2 antagonists, and an uterine contractile activity, a promoting effect of digestive peristalsis, a suppressive effect of gastric acid secretion, a hypotensive activity as PGE2 agonists, because they bind onto PGE2 receptor and have an activity of antagonist or agonist against the action thereof.

One aspect of the present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-sulfur bond between the sulfur atom of a thiol moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper(II)-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-carbon bond between the carbon atom of cyanide ion and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In another embodiment, the present invention relates to a copper-catalyzed method of transforming an aryl, heteroaryl, or vinyl chloride or bromide into the corresponding aryl, heteroaryl, or vinyl iodide. Yet another embodient of the present invention relates to a tandem method, which may be practiced in a single reaction vessel, wherein the first step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl iodide from the corresponding aryl, heteroaryl, or vinyl chloride or bromide; and the second step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl nitrile, amide or sulfide from the aryl, heteroaryl, or vinyl iodide formed in the first step.

The invention relates to a fluorination process for producing fluorinated compounds.The process consists in reacting a compound (I) corresponding to the formulawith an ionic fluoride of a monovalent cation. M represents H, an alkali metal, a quaternary phosphonium group or a quaternary ammonium group. Y represents SO2 and m is 1, or else Y is PO and m is 2. Z represents CR2, N or P. R1 represents an electron-withdrawing group which has a Hammet σP parameter of greater than 0.4. R2 represents a carbonaceous and / or electron-withdrawing group. X represents a halogen other than a fluorine.The fluorinated compounds obtained are of use in particular as electrolytes in lithium batteries.

The present invention provides compounds having formula (I):wherein R′, R0, R1, X1, R2, R3, R3′, X2, X3 and R4 are as defined herein, and pharmaceutical compositions thereof. The present invention also provides methods of inhibiting proteases, more specifically aspartyl proteases. In certain embodiments, compounds inhibit BACE (β-site APP-cleaving enzyme), and thus are useful in the treatment or prevention of a disease characterized by β-amyloid deposits in the brain (including, but not limited to, Alzheimer's Disease). The present invention also provides methods for preparing compounds of the invention.

A method for sequentially performing a synthesis, separation and screening of chemical entities, especially a combinatorial library, is described. The method utilises a bulk of a stationary phase (e.g. silica gel, aluminium oxide, cellulose, etc. for example arranged on a backing) for the performance of the synthesis, separation and screening. The technique described enables a rapid route from synthesis to the testing of chemical compounds. Screening can be performed without need for reaction work-up. Preferred screening methods are those used to determine the biological activity of the compounds.

A process for the preparation of a sulfonamide of formula (II), comprising reacting at elevated temperature an aniline of formula (I), with a sulfonating agent A of the formula R1—SO2-Z in the presence of a catalytic amount of either: (i) an amide B-1, other than N,N-dimethylformamide, or (ii) a high boiling tertiary amine B-2. Also provided in accordance with the present invention are processes for preparing sulfonamides of formula (II) by reacting an aniline of formula (I) with sulfanating agent A of the formula R1—SO2-Z in the presence of N,N-dimethylformamide, at a temperature in the range of about 120° C. to about 160° C. for about three to about seven hours. X, Y, Z, R and R1 are defined herein

The present invention provides a compound which is represented by a formula (A-I), a coloring curable resin composition with the compound, a color filter formed by the resin composition, and a display device with the color filter. In the formula (A-I), X represents an oxygen atom, a nitrogen atom or sulfur atom; [Y]m represents a random m-valued anion; R41-R46 independently represents hydrogen atom or an alkyl which can be substituted by an amino group or halogen atom and has 1-20 carbon atoms; R47-R54 independently represents a hydrogen atom, a halogen atom, a nitryl, a hydroxyl or an alkyl with 1-8 carbon atoms; and R55 represents a hydrogen atom, an alkyl with 1-20 carbon atoms or a substitutable aryl.

The present invention provides a compound represented by the formula:wherein R represents an aliphatic hydrocarbon group optionally having substituents, an aromatic hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, a group represented by the formula: OR1 (wherein R1 represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents) or a group represented by the formula:wherein R1b represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R1c is, same with or different from R1b, a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R0 represents a hydrogen atom or an aliphatic hydrocarbon group, or R and R0 represents a bond with each other, Ar represents an aromatic hydrocarbon group optionally having substituents,and n is an integer of 1 to 4, or a salt thereof, which is a agent for preventing or treating diseases such as cardiac disease, autoimmune disease, septick shock, etc.

The invention discloses a method for preparing bis(trifluoromethylsulfonyl)imide metallic salt. The method comprises the following steps: trifluoromethane halogenated sulfonyl, liquid ammonia and organic amine alkali as raw materials are used to generate a mixture solvent containing bis(trifluoromethylsulfonyl)imide quaternary ammonium salt by a nonpolar inert solvent; the mixture containing the bis(trifluoromethylsulfonyl)imide quaternary ammonium salt is distilled to reclaim the solvent so as to obtain a bis(trifluoromethylsulfonyl)imide quaternary ammonium salt solid; the bis(trifluoromethylsulfonyl)imide quaternary ammonium salt solid reacts with alkali metal oxide in an aqueous solution to generate a mixture of the bis(trifluoromethylsulfonyl)imide metallic salt; and finally, the target product is prepared by the obtained mixture of the bis(trifluoromethylsulfonyl)imide metallic salt through decompressed dehydrating, decompressed drying and other steps. The process has a simple route, and does not pollute the environment. The purity of the bis(trifluoromethylsulfonyl)imide metallic salt prepared by the method is more than 99 percent, and the yield is over 90 percent.

The invention relates to substituted sulphonamide compound and preparation method, medicine composition and application thereof, in particular provides the substituted sulphonamide compound shown in general formula (I) or pharmaceutically acceptable salt thereof, Ar, X, Y, Z and R are defined in the specification. The compound has good preventing and treating effect on diseases mediated by GPR40 such as diabetes, breast cancer and certain nerve disease. The compound is GTP bonding protein ion-channel-linked receptor 40 antagonist. Thus, the compound is hopeful to be developed into novel medicine for treating diabetes and the like. The invention also provides the preparation method and medicine composition of the compound.

The invention discloses a method for preparing binary or ternary fluorine-containing sulfimide alkali metal salts, a method for preparing ionic liquid by the binary or ternary fluorine-containing sulfimide alkali metal salts, and applications of the alkali metal salts and ionic liquid as electrolytes in carbon-based super capacitors, secondary lithium (ion) batteries, and the like. The method for preparing the binary or ternary fluorine-containing sulfimide alkali metal salts provided by the invention is short in operation steps, easy for product separation and purification, and high in product yield and purity; the binary or ternary fluorine-containing sulfimide lithium provided by the invention has good thermal stability and hydrolysis resistance; a nonaqueous electrolytic solution of the binary or ternary fluorine-containing sulfimide lithium has high conductivity and lithium ion transference number, and also exhibits good oxidation resistance and good compatibility with widely-used electrode materials; meanwhile, the ionic liquid containing the binary or ternary fluorine-containing sulfimide anions exhibits the properties of low viscosity and high conductivity, and has a wide electrochemical window.

The invention discloses alkali metal salts of binary or ternary fluorine-containing sulfimide, a method for preparing ionic liquid from the alkali metal salts of binary or ternary fluorine-containing sulfimide, and applications of the alkali metal salts and the ionic liquid as electrolytes in carbon-based supercapacitors, secondary lithium (ion) batteries, and the like. The method for preparing the alkali metal salts of binary or ternary fluorine-containing sulfimide provided by the invention is short in operation steps, and the product is easy to separate and purify, and very high in yield and purity; the binary or ternary fluorine-containing lithium sulfimide provided by the invention is good in thermal stability and hydrolysis resistance; the non-aqueous electrolyte has high conductivity and lithium ion transport number, exhibits good oxidation resistance, and has good compatibility with widely-used electrode materials; meanwhile, the ionic liquid containing binary or ternary fluorine-containing sulfimide anions is characterized by low viscosity and high conductivity, and has a wide electrochemical window.

The present invention provides amine derivatives represented by formula I, its isomers, racemes or optical isomers, pharmaceutical salts thereof, its amides or esters, pharmaceutical compositions containing said compounds and the preparation methods thereof. The invention also relates to the use of the above mentioned compounds in the preparation of drugs for the prophylaxis or treatment of cardiovascular diseases, diabetes, bronchial and urinary smooth muscle spasm as well as ischemic and anoxic nerve injury. The above compounds can be used to treat hypertension, angina diaphragmatic, myocardial infarction, congestive heart failure, arrhythmia, diabetes, spasmodic bronchial diseases, spasmodic bladder or ureter diseases, and depression.

The invention discloses a method for preparing bis(sulfonyl fluoride) imine and (perfluoroalkyl sulfonyl fluorine sulfonyl) imine alkali metal salt. According to the method, sulfamide is utilized to take reaction with thionyl chloride and chlorosulfonic acid for preparing bis(sulfonyl fluoride) imine or (perfluoroalkyl sulfonyl fluorine sulfonyl) imine, then, the bis(sulfonyl fluoride) imine or (perfluoroalkyl sulfonyl fluorine sulfonyl) imine takes reaction with antimony trifluoride and potassium (rubidium or caesium and the like) carbonate, and corresponding high-purity bis(sulfonyl fluoride) imine potassium (rubidium or caesium) salt or (perfluoroalkyl sulfonyl fluorine sulfonyl) imine potassium (rubidium or caesium) salt can be obtained; and the double decomposition exchange reaction of the potassium (rubidium or caesium) salt and lithium (or sodium) perchlorate or lithium (or sodium) tetrafluoroborate and the like in aprotic polar solvents is utilized to obtain corresponding high-purity lithium (or sodium) salt. The method provided by the invention has the characteristics that the operation step is simple, the products can be easily separated and purified, the purity and the yield are high, the environment pollution is avoided, the method is suitable for industrial mass production, and the like.

50 HMGCo-A reductase inhibitor compounds useful as hypocholesterolemic and hypolipidemic compounds are provided. Also provided are pharmaceutical compositions of the compounds. Methods of making and methods of using the compounds are also provided.