1647results 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:

wherein

• R1, 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; and
• B 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.

The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.

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 present invention provides compounds having formula (I):

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 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.

The invention discloses a preparation method for 2-amino sulfonyl-4-methylsalfonamido methyl benzoic acid methyl ester. According to the preparation method, sulfonamide methyl toluene is used as raw material and subjected to chlorosulfonation-ammonolysis reaction, oxidation reaction and methanolysis reaction to prepare the2-amino sulfonyl-4-methylsalfonamido methyl benzoic acid methyl ester, wherein in the chlorosulfonation reaction, sulfonamide methyl toluene and organic solvents are added to a reaction device to be cooled to minus 10 DEG C-0 DEG C via an ice bath, then chlorosulfonation reagents are dropwise added, next the mixtures are heated till reflux occurs and the reaction is complete. The preparation method disclosed by the invention can prepare 2-amino sulfonyl-4-methylsalfonamido methyl benzoic acid methyl ester by using sulfonamide methyl toluene as raw material via three reaction steps, greatly shortens the synthetic process, and is quite suitable for commercial process. The overall yield can reach above 50% by optimizing the chlorosulfonation-ammonolysis reaction condition.