1-((5,5-DIMETHYL-3-OXOCYCLOHEXENE-1-YL)AMINO)-3-PROPENE- 2-YLOXYPROPANOL-2 AS A MODIFIER OF SAWDUST FOR PURIFICATION OF SEWAGE FROM COPPER

Substituierte cyclische Ketone, substituierte cyclische Enone und Verfahren zu deren Herstellung

UNGESAETTIGTE KAMPFERDERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG AUF DEM GEBIET DER PHARMAZIE UND DER KOSMETIK

NOVEL 5-ACYL-2-(1H)-PYRIDINONES

Verfahren zur Herstellung von Ketonitril-Derivaten und Hexenon-Derivaten

Organic compounds

New cycloaliphatic ketoamines

There are prepared compounds of the formula: wherein X is the group >C=O or >CH(OH), Y is the group R2 is hydrogen or C1 to C6 alkyl, R3 is hydrogen or a hydroxy group and R1 is the adamantyl group or a saturated or single unsaturated C3 to C16 cycloalkyl group where the C3 to C16 cycloalkyl group can be substituted by a C1-C4 alkyl group or a halogen atom and their salts. The compounds are useful in dilating the peripheral blood vessels and in lowering blood pressure.

PROCEDURE FOR THE PRODUCTION OF SUBSTITUTING 1.1.1 - TRIFLUORO-3-BUTEN-2-ONE

ACETYLENE DERIVATIVES WITH ENZYMINHIBIERENDER EFFECT, THEIR PRODUCTION AND THEIR USE AS DRUGS.

5-ACYL-2 (1H) - PYRIDINONE.

NEW CARBACYCLINE, PROCEDURES FOR YOUR PRODUCTION AND YOUR USE AS DRUGS.

PROCEDURE FOR the PRODUCTION OF 3IMIDAZOLYLMETHYLTETRAHYDROCARBAZOLONEN.

5-ACYL-2 (1H) - PYRIDINONE.

RESOLVENTS

PHENYLETHYLAMINE AND RING-CONDENSED VARIANTS AS PRO DRUGS OF KATECHOLAMINEN AS WELL AS YOUR USE

IF CYCLI KETONE SUBSTITUTED, CYCLI ENONE AND PROCEDURE FOR THEIR PRODUCTION SUBSTITUTED

USE FROM PHENALKYLAMINEN TO THE PRODUCTION OF CHOLESTERINSENKENDEN DRUGS

NEW CARBACYCLINES, PROCESS FOR THEIR PRODUCTION AND THEIR USEAS MEDICAMENTS

Hexadentate ligands useful in radiographic imaging agents

SUBSTITUDED PYRIDYLPYRIMIDINES, THEIR PREPARATION AND THEIR USE, AS WELL AS NEW INTERMEDIATE PRODUCTS

Aminomethyl-phenyl-cyclohexanone derivatives

UNSATURATED CAMPHOR DERIVATIVES

LIGANDS FOR METALS AND METAL-CATALYZED PROCESSES

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 processes provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

PROCESS FOR PRODUCING 3-IMIDAZOLYLMETHYLTETRAHYDROCARBAZOLONES

The invention relates to a process for the preparation of a compound of general formula (I) (I) wherein R1 represents a hydrogen atom or a C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl-(C1-4)alkyl, C3-6 alkenyl, C3-10 alkynyl, phenyl or phenyl-(C1-3)alkyl group, and one of the groups represented by R2, R3 and R4 is a hydrogen atom or a C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl or phenyl-(C1-3)alkyl group and each of the other two groups, which may be the same or different, represent a hydrogen atom or a C1-6 alkyl group; or a salt or protected derivative thereof, by cyclisation of a compound of general formula (II) (II) wherein R1, R2, R3 and R4 are as defined above, or a salt or a protected derivative thereof. The compounds of formula (I) are potent and selective antagonists at "neuronal" 5-hydroxytryptamine receptors.

CYCLOALIPHATIC KETOAMINES

CONTRAST AGENT MADE OF A NEUTRAL COMPLEX OF PARAMAGNETIC CATION AND LIGAND TO MAKE A COMPLEX

BREVET D'INVENTION AGENT DE CONTRASTE CONSTITUE PAR UN COMPLEXE NEUTRE D'UN CATION PARAMAGNETIQUE ET LIGAND POUR FORMER UN COMPLEXE. Déposant: MEDGENIX GROUP S.A. La présente invention a pour objet un agent de contraste pour l'imagerie par RMN constitué d'un complexe de coordination neutre entre un ligand et un cation métallique, ou un hydrate de ce complexe, de formule : ML. mH2O (I) dans laquelle - M désigne un cation métallique paramagnétique trivalent - m est un entier de 0 à 5 - L est un ligand de formule: A-¢C(R1,R2)-(C(R?,R?))n-C(R3,R4)-N=C(R5)-C(R6)=C(R7)-O!3 (II) dans laquelle - A représente N ou C-R 10, - R1 à R 10' identiques ou différents, sont choisis parmi H, un hydroxyle, un halogène, un groupe alkyle, alcoxy, aryle, alkenyle, cycloalkyle groupes éventuellement substitués par un ou des groupes halogène, hydroxyle, alkyle, alcoxy, nitrile, nitro, amine, ou hydroxyalkyle. - n est un entier de 0 à 3, i est un entier de l à n. La présente invention a également pour objet un ligand ...

PROCESS FOR PRODUCING 4-TRIFLUOROMETHYLNICOTINIC ACID

A process for producing 4-trifluoromethylnicotinic acid of the formula (VIII) or its salt: (VIII) which comprises (i) a first step of reacting a halide of the formula (I): CF3COHal (I) wherein Hal is a halogen atom, with a compound of the formula (II): CH2=CHOR1 (II) wherein R1 is an alkyl group, in the presence of a base to obtain a 4-alkoxy-1,1,1-trifluoro-3-buten-2-one of the formula (III): CF3CO-CH=CH-OR1 (III) wherein R1 is as defined above, and reacting this compound with ammonia to obtain 4-amino-1,1,1-trifluoro-3-buten-2-one of the formula (IV): (IV) and (ii) a second step of subjecting the 4-amino-1,1,1-trifluoro-3-buten-2-one obtained in the first step and a compound of the formula (V): ACO2R2 (V) wherein R2 is an ester-forming residue, and A is (R3O)CH=CH- or (R3O)2CHCH2-, wherein R3 is an alkyl group, to a condensation reaction to obtain a compound of the formula (VI) (inclusive of its salt): (VI) wherein R2 is as defined above, and/or a compound of the formula ...

PROCESS AND INTERMEDIATES FOR THE PREPARATION OF EXCITATORY AMINO ACID RECEPTOR ANTAGONISTS

The present invention provides novel intermediates which are useful for the preparation of excitatory amino acid receptor antagonists. Further provided is a process to enatioselectively prepare hydroisoquinoline compounds with central nervous system activity.

USE OF PHENALKYLAMINES

Use of compounds of the formula (see formula I) wherein one of R1 and R2 is C1-7-alkyl and the other is C1-7-alkyl or C2-6-alkenyl-methyl, L is C1-11-alkylene or C2-11-alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene, n = 0 or, where L contains an O atom, n = 0 or 1; Q is C1-7-alkyl, C2-10-alkenyl or a group of formula Q': R is H, halogen, CF3, CN or NO2, R3 and R4 are H, C1-4-alkyl or halogen and R5 is H or, where R is H, H or halogen, and their pharmaceutically acceptable acid addition salts for the manufacture of cholesterol-lowering medicaments, as well as novel compounds falling under formula I.

CYCLO-ALIPHATIC AMINES, PROCEDURES FOR YOUR PRODUCTION AND THESE CONTAINING DRUGS.

CAMPHOR UNSATURATED DERIVATIVES, METHODS FOR THEIR PREPARATION AND PHARMACEUTICAL AND COSMETIC COMPOSITIONS CONTAINING THEM.

АНТИНЕОПЛАСТИЧЕСКИЕ КОМБИНАЦИИ

Настоящее изобретение относится к применению комбинации CCI-779 и ЕКВ-569 для лечения новообразований.

Organic compounds

The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula (VI), or a salt thereof, wherein R<1>, R<2>, R<3> and R' are as defined in the specification, and processes of manufacturing this compound including intermediates.

Preparation method for synthesizing alpha-aminoketone compound from fatty aldehyde and secondary amine

The invention discloses a preparation method for synthesizing an alpha-aminoketone compound from fatty aldehyde and secondary amine, and belongs to the technical field of organic chemical synthesis, fatty aldehyde, secondary amine and sodium percarbonate are added into a reaction container to be mixed and react for 16-24 hours at the temperature of 95-115 DEG C, and the alpha-aminoketone compound is obtained after the reaction mixture is purified. The fatty aldehyde and the secondary amine used in the method are prepared from commercially available raw materials or commercially available primary alcohol and primary amine through simple oxidation or reduction; the method is simple, the substrate application range is wide, the method is suitable for various fatty aldehydes and secondary amines, the method can be used for preparing the fatty aldehydes and secondary amines only by oxidizing and rearranging the cheap and easily available sodium percarbonate, additional catalysts and additives ...

USE Of a DRIFT Of ACID (DIHYDRO) JASMONIQUE FOR the TREATMENT OF the PEAUXSECHES

Agent of contrast consisted a neutral complex of a paramagnetic cation and ligand to form uncomplexe

La présente invention a pour objet un agent de contraste pour l'imagerie par RMN constitué d'un complexe de coordination neutre entre un ligand et un cation métallique, ou un hydrate de ce complexe, de formule: (CF DESSIN DANS BOPI) dans laquelle - M désigne un cation métallique paramagnétique trivalent - m est un entier de 0 à 5 - L est un ligand de formule: (CF DESSIN DANS BOPI) dans laquelle - A représente N ou C-R1 0 , - R1 à R1 0 , identiques ou différents, sont choisis parmi H, un hydroxyle, un halogène, un groupe alkyle, alcoxy, aryle, alkenyle, cycloalkyle groupes éventuellement substitués par un ou des groupes halogène, hydroxyle, alkyle, alcoxy, nitrile, nitro, amine, ou hydroxyalkyle. - n est un entier de 0 à 3, i est un entier de 1 à n. La présente invention a également pour objet un ligand pouvant former des complexes de coordination avec des cations métalliques trivalents, caractérisé en ce qu'il répond à la formule: (CF DESSIN DANS BOPI) et un procédé de préparation de ces ...

PRO-FRAGRANCES

The present invention relates to fragrance delivery systems which comprise: a) one or more pro-fragrances having formula (I) wherein G?1 and G2¿ are methyl, or a cyclic hydrocarbyl unit derived from the isomers of ionone and/or damascone; R and R1 are each independently C¿1?-C22 substituted or unsubstituted, branched or unbranched alkyl, C2-C22 substituted or unsubstituted, branched or unbranched alkenyl, C2-C20 substituted or unsubstituted, branched or unbranched hydroxyalkyl, C7-C20 substituted or unsubstituted alkylenearyl, C3-C20 substituted or unsubstituted cycloalkyl, alkyleneoxy; C6-C20 aryl, C5-C20 heteroaryl comprising one or more heteroatoms selected from the group consisting of nitrogen, oxygen, sulfur, and mixtures thereof; two of the units Y?1, Y2¿, R or R1 can be taken together to form one or more aromatic or non-aromatic, heterocyclic or non-heterocyclic, single rings, fused rings, bicyclo rings, spiroannulated rings, or mixtures thereof, said rings comprising from 3 to 20 carbon atoms and one or more heteroatoms selected from the group consisting of nitrogen, oxygen, sulfur, and mixtures thereof; b) one or more aldehyde releasing oxazolidine pro-fragrances; and c) the balance carriers, pro-fragrances, pro-accords, other perfume ingredients.

Ｎ−置換ピリジニウム化合物の調製のための方法および物質

PRODUCTION OF NEOCARZIRINS

PURPOSE: To efficiently produce the subject compounds useful as an anti- neoplastic agent, etc., by a ready operation by reacting a specified carboxylic acid with a ketone compound synthesized through a reaction between a specified alcohol and triphenylphosphoranylidenepropanone in the presence of a strong base. CONSTITUTION: An alcohol of formula I (R1 is lower alkyl, tetrahydropyranyloxyethyl, etc.; n is 1 or 2) is reacted with triphenylphosphoranylidene-2-propanone and the resultant ketone compound of formula II is reacted with a carboxylic acid of formula R2COOH [R2 is (halogen-substituted) lower alkyl] or its reactive derivative in the presence of a strong base such as sodium hexamethyldisilazane, thus obtaining the objective compounds of formula III. COPYRIGHT: (C)1993,JPO&Japio ...

АЛКИЛАМИНОКЕТОНЫ

Описываются новые соединения общей формулы I, где значения R1, m , R2, L, R3, Q указаны в п.1 формулы изобретения. Соединения формулы I и их соли обладают эффективным действием по снижению содержания холестерина в крови, и поэтому могут применяться для борьбы и профилактики гиперхолестеринемии и атеросклероза, обусловливающих большую часть сердечно-сосудистых заболеваний. 1 з.п. ф-лы, 2 табл.

Способ получения пергалоидалкил-бета-диэтиламиновинилкетонов

Способ получения циклоалифатических кетоаминов или их солей

Способ получения этиленовых оксиаминокетонов

Способ получения циклоалифатических кетоаминов или их солей

RIECHSTOFFVORSTUFEN

CYCLOYLIPHATIC KETOAMINES

6-ALKYL-1,2-DIHYDRO-2-OXOPYRIDINE DERIVATIVES

Silver halide photographic light-sensitive material

A silver halide photographic light-sensitive material is disclosed. The material is comprised of a support having thereon a light-sensitive silver halide layer and a light-insensitive layer. The material may also contain other layers and one or more layers contains an ultraviolet ray absorbing polymer latex. The polymer latex is comprised of a homopolymer or a copolymer having a repeating unit derived from a monomer represented by the following general formula (I): (I) within the general formula (I) the Q represents an ultraviolet ray absorbing group represented by the general formula (II): (II) the substituents within the general formulae (I) and (II) are defined in a specification. The photographic light-sensitive material has excellent absorbing characteristic in the 300 to 400 nm range and does not cause static marks caused by ultraviolet layer. Furthermore, the material does not undergo discoloration. In addition, the photographic material has good film strength and a reduced layer ...

2-AMINO-1, 3 - PROPANDIOLVERBINDUNG AND IMMUNOSUPPRESSIUM

PROCEDURE FOR THE PRODUCTION OF ALPHA ((DIALKYLAMINO) SUBSTITUTING SUBSTITUIERTES-METHYLEN) - BETA-OX - (SUBSTITUTED) - PROPANE NITRILES.

AMINOMETHYL PHENYL CYCLOHEXANONDERIVATE ONE

BENZENE DERIVATIVES, YOUR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS, THIS CONTAINING.

MULTI-FULL OF SEEDS SUBSTITUTED COMPLEXING AGENTS, COMPLEXES AND COMPLEX SALTS, PROCEDURES FOR THEIR PRODUCTION AND THESE CONTAINING PHARMACEUTICAL MEANS.

Bicyclic quinone compounds, their production and use

PROPENYL-AMINES, PROCESSES FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

PROCESS FOR PRODUCING 4-TRIFLUOROMETHYLNICOTINIC ACID

A process for producing 4-trifluoromethylnicotinic acid of the formula (VIII) or its salt: (see formula I) which comprises (i) a first step of reacting a halide of the formula (I): CF3COHal (I) wherein Hal is a halogen atom, with a compound of the formula (II): CH2=CHOR1 (II) wherein R1 is an alkyl group, in the presence of a base to obtain a 4-alkoxy-1,1,1-trifluoro-3-buten-2-one of the formula (III): CF3CO-CH=CH-OR1 (III) wherein R1 is as defined above, and reacting this compound with ammonia to obtain 4-amino-1,1,1-trifluoro- 3-buten-2-one of the formula (IV): and (ii) a second step of subjecting the 4-amino-1,1,1- trifluoro-3-buten-2-one obtained in the first step and a compound of the formula (V): ACO2R2 (V) wherein R2 is an ester-forming residue, and A is (R3O)CH=CH- or (R30)2CHCH2-, wherein R3 is an alkyl group, to a condensation reaction to obtain a compound of the formula (VI) (inclusive of its salt): wherein R2 is as defined above, and/or a compound of the formula ...

PROCESS FOR THE PREPARATION OF SUBSTITUTED KETO-ENAMINES

The present invention discloses a process for the preparation of a substantially pure compound having formula (4). The process comprises the step of reacting an enolate having formula (A) with a Grignard reagent. The enolate salt is formed in situ from the reaction of a protected ester wherein M is an alkali metal. R6 and R7 are each hydrogen or are independently selected from (i) wherein Ra and Rb are independently selected from hydrogen, lower alkyl and phenyl and Rc, Rd and Re are independently selected from hydrogen, lower alkyl, trifluoromethyl, alkoxy, halo and phenyl; and (ii) wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents independently selected from lower alkyl, trifluoromethyl, alkoxy and halo. Alternatively, R6 is as defined above and R7 is R12OC(O)- wherein R12 is benzyl; or R6 and R7 taken together with the nitrogen atom to which they are bonded form (B) or (C), wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, lower alkyl, alkoxy, halogen and trifluoromethyl.

PROCESS FOR CONVERTING PROPARGYLIC AMINE-N-OXIDES TO ENAMINONES

This invention concerns the use of a hydroxylic solvent in the preparation of enaminones from the corresponding amine N-oxides or propargylic amines via the general process outlined above (A).

IODOPROPAGYLAMINE COMPOUNDS, AND INDUSTRIAL ANTIMICROBIAL AND ANTIFUNGAL AGENTS, ALGICIDES, AND ANTIFOULING AGENTS CONTAINING THE SAME

Iodopropagylamine compounds represented by general formula (1) (wherein R1 and R2 each independently represent a hydrogen atom or a 1-3 C alkyl group, or R1 and R2 combine with each other to form a tetramethylene or pentamethylene group; R3 represents a hydrogen atom or a 1-3 C alkyl group; X and Y each independently represent a cyano group, a 2-7 C alkoxycarbonyl group, a 2-7 C alkylcarbonyl group, a 1-6 C alkylsulfonyl group, a phenylcarbonyl group, or a phenylsulfonyl group, provided that the phenyl group of a phenylcarbonyl group or a phenylsulfonyl group may be optionally substituted by a halogen atom, a 13 C alkyl group, a 1-3 C alkoxy group, a nitro group, or a trifluoromethyl group). The compounds are useful as the active ingredient for industrial antimicrobial and antifungal agents, algicides, and antifouling agents.

СПОСОБЫ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ 4-N,N-ДИМЕТИЛАМИНОКРОТОНОВОЙ КИСЛОТЫ

Настоящее изобретение относится к способам получения производных 4-N,N-диметиламинокротоновой кислоты, в частности к способу получения [4-(3-хлор-4-фторфениламин)-3-циан-7-этоксихинолин-6-ил]амидом 4-диметиламинобут-2-еновой кислоты (ЕКВ-569).

Novel enamine compound and preparation method and medical application thereof

NOUVEAUX COMPOSES A LA PYRIDINE ET COMPOSITION PHARMACEUTIQUE LES CONTENANT

L'INVENTION A TRAIT AU DOMAINE DE LA CHIMIE PHARMACEUTIQUE. ELLE CONCERNE CERTAINS ACIDES 1,2-DIHYDRO-2-OXO-6-ALKYL-3-PYRIDINE-CARBOXYLIQUES, LEURS ESTERS ET LEURS METHANOLS, DE FORMULE: (CF DESSIN DANS BOPI) DANS LAQUELLE R REPRESENTE H, CH OU CH; R REPRESENTE COR OU -CHOH, R EST L'HYDROGENE OU UN GROPUE ALKYLE EN C A C ET R EST UN RADICAL ORGANIQUE. LES COMPOSES DE L'INVENTION SONT DOUES D'ACTIVITE ANTIHYPERGLYCEMIQUE.

[...] CYCLOALIPHATIC, PREPARATION AND THERAPEUTIC USES

2-ARYLOXY-2-PROPEN-1-ONE DERIVATIVES

Method for preparing Asymmetric betaketoiminate ligand compound

α,α-디할로아민 및 케트이민으로부터 3,5-비스(할로알킬)피라졸 유도체의 제조방법

... 본 발명은 α,α-디할로아민 및 케트이민으로부터 3,5-비스(할로알킬)피라졸 유도체의 신규 제조방법에 관한 것이다.

2,4-DIHYDROXYL CHALCONE DERIVATIVE, PROCESS FOR PREPARING THEM AND USE THEREOF

Disclosed is a new 2,4-dihydroxyl chalcone derivative having the structure of general formula i and a pharmaceutically acceptable salt thereof, in which each group has the same meaning as defined in the specification, and a process for preparing them, a pharmaceutical composition comprising them, and their use of anti-tumor.

THIN FILM-FORMING MATERIAL, THIN FILM, AND THIN FILM PRODUCING METHOD

Provided is a thin film-forming material containing a yttrium compound represented by general formula (1). (In the formula, R1 and R3 each independently represent an alkyl group having 1-6 carbon atoms or an alkoxyalkyl group having 2-6 carbon atoms, R2 represents a hydrogen atom or an alkyl group having 1-3 carbon atoms, R4 represents an alkanediyl group having 1-5 carbon atoms, R5 represents an alkyl group each having 1-3 carbon atoms, and R1, R2, R3, R4, and R5, which are each present in a number of more than one, may be the same or different within each other.) ...

PROCESS FOR PRODUCING PYRROLE COMPOUND

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

SYNTHETIC ION CHANNELS

PREPARATION OF BETA-ACYLENAMINE

PURPOSE: To obtain the titled compound useful for synthesizing alkaloid, by condensing an oxime sulfonate with a silyl enol ether in the presence of a reagent. CONSTITUTION: An oxime sulfonate shown by the formula I (R1 and R2 are H, or 1W30C hydrocarbon which may contain N, O, P, or S; R3 is 1W20C hydrocarbon) is condensed with a silyl enol ether shown by the formula II (R4WR6 are H, 1W 30C hydrocarbon which may contain N, O, P, or S; R7WR9 are 1W 20C hydrocarbon) in the presence of a reagent [e.g., RnAlX3-n(R is 1W20C hydrocarbon; X is H, or halogen, etc.; 0≤n≤3)] to give a β-acylenamine shown by the formula III. A blending ratio of oxime sulfonate, silyl enol ether and the reagent is (1:0.1: 0.1)W(1:5:20), and the condensation reaction is carried out in an inert solvent by taking handling of the reagent into consideration. COPYRIGHT: (C)1984,JPO&Japio ...

СОЕДИНЕНИЯ ДЛЯ КОНТРОЛИРУЕМОГО ВЫСВОБОЖДЕНИЯ АКТИВНЫХ МОЛЕКУЛ

Настоящее изобретение относится к области парфюмерии. В особенности оно относится к ароматизирующей композиции, содержащей в качестве активного ингредиента, по крайней мере, соединение формулы где значения для w, m, P, X, G, Q, n определены в п.1 формулы, и один или более ароматизирующий соингредиент. Изобретение также относится к способу улучшения, усиления или модификации запаха, способу ароматизирования поверхности, способу усиления или продления диффузионного эффекта ингредиента на поверхности, к новым соединениям формулы (I), за исключением соединений, перечисленных в п.10 формулы, и к ароматизированному изделию с использованием соединений формулы (I). 6 н. и 7 з.п. ф-лы.

4,5-Диметил-7-гидрокси-5-азагептен-3-он-2 в качестве модификатора древесных опилок для очистки сточных вод от меди

Сущность изобретения: продукт: 4,5-ди- метил-7-гидрокси-5-азагептен-3-ОН/2, НО- СН2-СН2-М(СНз)-С(СНз) СН-С(0)-СНз, БФ CsHi5N02, выход 78,8%, т.пл. 84-85°С. Реагент 1: ацетилацетон. Реагент 2: 2-(метила- мино)этанол, Условия реакции: в среде бензола при т,кип. реакционной смеси. 2 табл.

Способ получения енаминов

Способ получения N-бета,бета,бета-трихлор-альфа-этилолацилвиниламинов

СПОСОБ ПОЛУЧЕНИЯ ЕН-ДИ-(β-ХЛОРЭТИЛ)-АМИНОВ

MEHRKERNIGE SUBSTITUIERTE KOMPLEXBILDNER, KOMPLEXE UND KOMPLEXSALZE, VERFAHREN ZU DEREN HERSTELLUNG UND DIESE ENTHALTENDE PHARMAZEUTISCHE MITTEL

NEW CARBACYCLINE, PROCEDURES FOR YOUR PRODUCTION AND YOUR USE AS DRUGS.

PROCEDURE FOR the PRODUCTION OF 3IMIDAZOLYLMETHYLTETRAHYDROCARBAZOLONEN.

PROCEDURE FOR THE PRODUCTION OF 4 - TRI FLUORINE METHYL NICOTINE ACID

SECHSBINDIGE LIGANDS FOR RADIO-GRAPHIC ILLUSTRATION AGENTS

ENAMINE AS VULCANIZING ACCELERATORS FOR NATUR-UND SYNTHETIC INDIA RUBBERS

SMELLING OFF PRELIMINARY STAGES

PROCEDURE FOR THE PRODUCTION OF 4 - HALO ALKYL NICOTINE ACID ESTERS

PROCEDURE FOR THE PRODUCTION OF NEW AMINES AND THEIR SALTS

Process for producing particles of amine reaction product

Process for converting propargylic amine-N-oxides to enaminones

HYDROXYLATED ENE KETONES, ACETYLENIC GRIGNARDS AND HYDROXYLATED YNE KETONES THEREFROM

CARBACYCLINS, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS

PROCESS FOR PRODUCING A TRIFLUORO-3-BUTEN-2-ONE COMPOUND

A process for producing a 4-alkoxy-1,1,1- trifluoro-3-buten-2-one of the formula (III): CF3CO-CH=CH-OR1 ~(III) wherein R1 is an alkyl group, or 4-amino-1,1,1- trifluoro-3-buten-2-one of the formula (IV): CF3-CO-CH=CH-NH2 ~(IV) which comprises (i) a first step of reacting a halide of the formula (I): CF3COHal~ (I) wherein Hal is a halogen atom, with a compound of the formula (II): CH2=CHOR1 ~(II) wherein R1 is as defined above, in the presence of a base to obtain the 4-alkoxy-1,1,1-trifluoro-3-buten-2-one and if required, further reacting this compound with ammonia to obtain 4-amino-1,1,1-trifluoro-3-buten-2-one.

2-AMINO-1,3-PROPANEDIOL COMPOUND AND IMMUNOSUPPRESSANT

SUBSTITUTE REMPLACEMENT SECTION is not Present Cette Section est Absente ...

BICYCLIC QUINONE COMPOUNDS, THEIR PRODUCTION AND USE

A compound of formula (I), wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from -X-Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.

Synthetic ion channels

Provided herein are self-assembling compounds that can form ion channels in lipid bilayers or cell membranes and ion-channel-forming compositions comprising the self-assembling compounds. Also provided are methods of making and using the ion channels formed from a plurality of molecules of the self-assembling compounds. Further, provided are methods of treating or preventing conditions and diseases that are related to the dysfunction of ion channels, including chloride channels.

Houttuynia cordata derivatives and applications thereof in drug

The invention relates to houttuynia cordata derivatives or esters thereof, or an enantiomer or a diastereomer, stereomer, tautomer, hydate, solvate, predrug, or pharmaceutically acceptable salt. In addition, the invention further relates to a preparation method of the houttuynia cordata derivatives, and an application of the houttuynia cordata derivatives in a drug; and the invention further relates to a pharmaceutical composition of the compound, and applications in preparing an antibacterial and anti-virus drug especially used for treating various urinary system diseases, and the advantages are that the water solubility is good, the bioavailability is high, the purity is high, and the toxic and side effects and the stimulation effect due to low purity can be greatly reduced.

PROCESS FOR PREPARING 5-ACYL-2-(1H)-PYRIDINONES

... 5-Acyl-2-(1H)-pyridones of formula (I) and pharmaceutically acceptables salt are prepd. by reacting a 1-R5-3-R6-2- (1dimethylamino-1-R4-methylidenyl)-1,3-propane-dione with an x- substd. acetoacetamide. In the formula, R3 is H, -C=N, NH2, CONH2 or COOR (R is H or lower alkyl); R4 is H or lower alkyl; R5 is phenyl, xsubstd. phenyl, pyridyl, thienyl, furyl, pyrrolyl or OR (R is H or lower alkoxy; X is lower alkyl, alkoxy, alkylthio, halogen, nitro, lower alkanoyl, alkoxy carbonyl, carboxy, cyano, NH2, CONH2, amidino, imidazol-2-yl or (F3); R6 is H, methyl, ethyl orR5. (I) are cardiotonics used in treatment of cardiac failure. Copyright 1997 KIPO ...

METHOD FOR PREPARING PYRAZOLECARBOXYLIC ACID DERIVATIVE, AND INTERMEDIATE THEREOF

Provided are a preparation method for synthesizing a pyrazolecarboxylic acid derivative of the following formula (I), which is suitable for industrial production, and an intermediate as shown by the following formula (II). The method is high in reaction yield in each step, low in waste gas and waste water and low in cost, and requires no special reaction equipment.

PROTEIN KINASE C MODULATORS WITH ANTI-INFLAMMATORY AND ANTIVIRAL ACTIVITY

Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from diterpenes, aromatic heterocyclic compounds of the indole, indene, benzofuran and benzothiophene class and from polyacetates, diaminobenzyl alcohols, diacylglycerols and bryostatins.

SUBSTITUTED CYCLIC KENTONES, SUBSTITUTED CYCLIC ENONES

PLANT ACTIVATOR

A compound useful as a plant activator for activating an endogenous defense system of a plant to control disease damage is provided. A compound represented by the formula: (R)NH—(CH)—N(R)—(CH)—NH(R) (one of Rand Rrepresents a linear Calkanoyl group or alkenoyl group, the other represents hydrogen atom or a protective group of amino group; and Rrepresents hydrogen atom or a protective group of amino group). 1. A compound represented by the following general formula (I): (R)NH—(CH)—N(R)—(CH)—NH(R) (In the formula , one of Rand Rrepresents a linear alkanoyl group having 6 to 18 carbon atoms or a linear alkenoyl group having 6 to 18 carbon atoms (the linear alkanoyl group and the linear alkenoyl group may have 1 to 3 hydroxyl groups , and/or 1 to 3 alkyl groups having 1 to 4 carbon atoms) , the other represents hydrogen atom or a protective group of amino group; and Rrepresents hydrogen atom or a protective group of amino group) , or a salt thereof.2. The compound or a salt thereof according to claim 1 , wherein one of Rand Ris a linear alkanoyl group having 8 to 13 carbon atoms or a linear alkenoyl group having 8 to 13 carbon atoms (the linear alkanoyl group and the linear alkenoyl group may have 1 to 3 hydroxyl groups) claim 1 , the other is hydrogen atom or a protective group of amino group claim 1 , and Ris hydrogen atom or a protective group of amino group.3. The compound or a salt thereof according to claim 1 , wherein one Rand Ris a linear alkanoyl group having 8 to 13 carbon atoms (the linear alkanoyl group may have 1 to 3 hydroxyl groups) claim 1 , the other is hydrogen atom or a protective group of amino group claim 1 , and Ris hydrogen atom or a protective group of amino group.4. The compound or a salt thereof according to claim 1 , wherein the linear alkanoyl group is a linear alkanoyl group having 9 to 12 carbon atoms (the linear alkanoyl group may have 1 or 2 hydroxyl groups).5. The compound or a salt thereof according to claim 1 , wherein the linear ...

CHOLINE ANALOGS AND CHEMICAL SYNTHESIS THEREOF

A method of making a betaine aldehyde, comprising ozonizing an allyl trimethylammonium to form the betaine aldehyde. 1. A method of making a betaine aldehyde , comprising ozonizing an allyl trimethylammonium to form the betaine aldehyde.2. The method of claim 1 , wherein the nitrogen atom of the allyl trimethylammonium is isotopically enriched N.3. The method of claim 1 , wherein at least one of the hydrogen atoms of the allyl trimethylammonium is istopically enriched D.4. The method of claim 1 , wherein the allyl trimethylammonium is an allyl trimethylammonium chloride or an allyl trimethylammonium bromide.5. The method of claim 1 , wherein the ozonizing step comprises reacting the ally trimethylammonium with ozone to form a peroxide claim 1 , and reducing the peroxide with dimethyl sulfide to form the betaine aldehyde.6. The method of claim 1 , further comprising synthesizing the allyl trimethylammonium from a trimethylammonium and an allyl.7. The method of claim 6 , wherein the nitrogen atom of the trimethylammonium is isotopically enriched N.8. The method of claim 6 , wherein at least one of the hydrogen atoms of the trimethylammonium is istopically enriched D.9. The method of claim 6 , wherein the trimethylammonium is a trimethylammonium bromide or a trimethylammonium chloride.10. The method of claim 6 , wherein at least one of the hydrogen atoms of the allyl is isotopically enriched D. This patent application is a continuation of U.S. application Ser. No. 13/405,074 filed Feb. 24, 2012, which claims priority to U.S. Provisional Patent Application No. 61/446,391 filed Feb. 24, 2011. The entire content of each of these applications is hereby incorporate by reference.This invention was made with government support under National Institutes of Health grant numbers 1R00CA134749 and 3R00CA134749-02S1. The government has certain rights in the invention.Hyperpolarized MRI offers a sensitivity increase by 4-6 orders of magnitude as compared to conventional MRI. ...

NOVEL STEREOSPECIFIC SYNTHESIS OF (-) (2S, 3S)-1-DIMETHYLAMINO-3-(3-METHOXYPHENYL)-2-METHYL PENTAN-3-OL

The present invention relates to a novel stereospecific synthesis of (−)(2S,3S)-1-dimethylamino-3-(3-methoxyphenyl)-2-methyl pentan-3-ol an intermediate in the synthesis of 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol. 18-. (canceled)10. The process of wherein the solvent employed is selected from the group consisting of ethers claim 9 , halo carbonated solvents claim 9 , and esters.11. The process of wherein the ether is selected from the group consisting of tetrahydrofuran (THF) claim 10 , 1 claim 10 ,4-dioxane claim 10 , diethyl ether or mixtures thereof.12. The process of wherein the halo carbonated solvent is selected from the group consisting of methylene chloride claim 10 , ethylene dichloride claim 10 , chloroform claim 10 , chlorobenzene claim 10 , dichlorobenzene and mixtures thereof.13. The process of wherein the ester is selected from the group consisting of ethyl acetate claim 10 , isopropyl acetate claim 10 , n-butyl acetate claim 10 , tert-butyl acetate and mixtures thereof.14. The process of wherein the solvent is tetrahydrofuran.15. The process of wherein the reaction is performed at a temperature from about 0° C. to about 100° C.16. The process of wherein the reaction is performed at the boiling point of the solvent(s) used.17. The process of wherein the reaction is performed at about 25° C.18. The process of wherein the reaction is carried out at a time period from about 15 minutes to about 10 hours.19. The process of wherein the reaction is carried out at a time period from about 30 minutes to about 2 hours.20. The process of wherein the molar equivalent of the compound of formula IV and reagent used is from about 0.25 to about 7 molar equivalents on the weight of the compound of formula V.21. The process of wherein the molar equivalent of the compound of formula IV and reagent used is about 1 molar equivalent on the weight of the compound of formula V.22. The process of wherein the compound of the formula III obtained has a purity ...

Abuse-Deterrent Methadone for the Safe Treatment of Drug Abuse and Pain Relief

Provided is a drug substance and a method of treating an ailment comprising administering an oral dose of a drug product comprising the drug substance wherein the drug substance comprises an organic acid addition salt of methadone. The organic acid addition salt is selected from the group consisting of pamoate and xinafoate wherein the drug substance is bioavailable under gastrointestinal administration but is not bioavailable under administration at a mucosal membrane other than gastrointestinal or release from a depot injectable product. 1. A drug substance comprising an organic acid addition salt of methadone wherein said organic acid addition salt is selected from the group consisting of pamoate and xinafoate.2. The drug substance of wherein said organic acid addition salt is pamoate.3. The drug substance of wherein said drug substance is methadone pamoate 2:1.4. The drug substance of wherein said methadone pamoate 2:1 is amorphous.5. The drug substance of wherein said amorphous methadone pamoate is characterized by at least one method selected from the group consisting of:{'figref': {'@idref': 'DRAWINGS', 'FIG. 5'}, 'a differential scanning calorimetry thermogram of indicating a phase transition of at least 0.4 W/g at 225-275° C.;'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 6'}, 'a fourier transform infrared spectrum of ; and'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 7'}, 'a powder x-ray diffraction diffractogram of .'}6. The drug substance of wherein said drug substance is methadone pamoate 1:1.7. The drug substance of wherein said methadone pamoate 1:1 is polymorphic.8. The drug substance of wherein said polymorphic methadone pamoate is characterized by at least one method selected from the group consisting of:{'figref': {'@idref': 'DRAWINGS', 'FIG. 9'}, 'a differential scanning calorimetry thermogram of indicating a phase transition of at least 1.5 W/g at 200-230° C. and a phase transition of at least 1.0 W/g at 240-260° C.;'}{'figref': {'@idref': 'DRAWINGS', ' ...

POLYMORPHS OF BROMFENAC SODIUM AND METHODS FOR PREPARING BROMFENAC SODIUM POLYMORPHS

Different polymorphs of bromfenac sodium may be prepared and interconverted using crystallization/recrystallization, drying and/or hydration techniques. 1. Bromfenac sodium Form III , characterized by a powder x-ray diffraction pattern having a main peak expressed as 2-theta at about 21.6 degrees.2. Bromfenac sodium Form III in accordance with claim 1 , characterized by a powder x-ray diffraction pattern having additional main peaks expressed as 2-theta at about 22.4 claim 1 , 12.2 claim 1 , 24.0 and 26.3 degrees.3. Bromfenac sodium Form III in accordance with claim 1 , characterized by a powder x-ray diffraction pattern having additional main peaks expressed as 2-theta at about 12.4 claim 1 , 14.1 claim 1 , 17.8 claim 1 , 19.6 claim 1 , and 28.1 degrees.4. Bromfenac sodium Form III in accordance with claim 1 , substantially free of any other physical forms of bromfenac sodium.5. Bromfenac sodium Form III in accordance with claim 1 , characterized by a powder x-ray diffraction pattern substantially in accordance with that shown in FIG.6. Bromfenac sodium Form III in accordance with claim 1 , characterized by an FT-IR spectrum substantially in accordance with that shown in .7. Bromfenac sodium Form III in accordance with claim 1 , characterized by an XRPD d-spacing/% intensity pattern substantially in accordance with that shown in Table B.8. A method of preparing bromfenac sodium Form III claim 1 , comprising crystallizing or recrystallizing bromfenac sodium from a solvent mixture comprising water and at least one alcohol.9. The method of claim 8 , wherein the at least one alcohol includes at least one C-Calcohol.10. The method of claim 8 , wherein the bromfenac sodium has been produced by hydrolysis of 7-(4-bromobenzoyl)indol-2-one and the solvent mixture is additionally comprised of at least one aromatic hydrocarbon and at least one anti-solvent.11. The method of claim 8 , wherein the solvent mixture is comprised of water and 2-propanol or is comprised of water ...

CF3O-CONTAINING ENAMINOKETONES AND THEIR UTILIZATION FOR THE PREPARATION OF CF3O-CONTAINING PYRAZOLES

The present invention pertains to novel enaminoketones containing a CFO-group, novel pyrazole-derivatives containing a CFO group as well as to a novel process for their preparation comprising aminoformylation of CFO-ketones and cyclization of the obtained CFO-enaminoketones with hydrazines to trifluoromethoxy pyrazoles. 2. Process according to claim 1 , wherein{'sup': '1', 'Ris 2-furyl, phenyl, or phenyl substituted with one or two chlorine atoms and'}{'sup': 2', '3, 'sub': 1', '6, 'Rand Rare independently C-Calkyl.'}6. Process according to claim 1 , wherein (A) is performed at a temperature of from 50° C. to 150° C.7. Process according to claim 1 , wherein the (A) is performed in a solvent selected from DMF claim 1 , toluene claim 1 , xylenes claim 1 , chlorobenzenes claim 1 , and dimethylacetamide.8. Process according to claim 2 , wherein (B) is performed at a temperature of from 0° C. to 50° C.10. Process according to claim 9 , wherein the compound of formula V-1 is oxidized using an oxidant selected from RuCl/NaIO claim 9 , RuO claim 9 , O claim 9 , KMnO claim 9 , and CrO.11. Process according to claim 9 , wherein the process is performed in a solvent selected from hexane/AcOEt/HO claim 9 , CCl/CHCN/HO claim 9 , HO/MeCN/AcOEt claim 9 , and HO/CHCl/MeCN. The present invention pertains to novel enaminoketones containing a CFO-group, novel pyrazole-derivatives containing a CFO group as well as to a novel process for their preparation comprising aminoformylation of CFO-ketones and cyclization of the obtained CFO-enaminoketones with hydrazines to trifluoromethoxy pyrazoles.Fluorine as a substituent in active ingredients plays a significant and increasingly important role. The biggest group of fluorinated pesticides are the compounds containing a trifluoromethyl group (mainly in aromatic rings), followed by aromatic compounds containing at least one isolated fluorine atom. Only five pesticides contain OCF-groups are on the market. It was estimated that the number of ...

HALOGEN SUBSTITUTED DIKETONES, PYRAZOLE COMPOUNDS AND PROCESSES FOR THE MANUFACTURE OF PYRAZOLE COMPOUNDS

The present invention concerns new halogen substituted diketone compounds, new pyrazole compounds, processes for the manufacture of pyrazole compounds and processes for the manufacture of agrochemical or pharmaceutical compounds. 2. The compound according to claim 1 , wherein Ris selected from the group consisting of CCl3 claim 1 , CF3 claim 1 , CBr3 claim 1 , and CI.3. The compound according to claim 1 , wherein{'sup': 1', '2', '4', '5, 'sub': 2', '3, 'Ris CFCl, Y is O, Ris CCl, Ris H, Ris ethyl or'}{'sup': 1', '2', '4', '5, 'sub': 2', '3, 'Ris CFCl, Y is O, Ris CF, Ris H, Ris ethyl or'}{'sup': 1', '2', '4', '5, 'sub': 2', '3, 'Ris CFH, Y is O, Ris CCl, Ris H, Ris ethyl or'}{'sup': 1', '2', '4', '5, 'sub': 2', '3, 'Ris CFH, Y is O, Ris CF, Ris H, Ris ethyl or'}{'sup': 1', '2', '4', '5, 'sub': 2', '3, 'Ris CFH, Y is O, Ris CBr, Ris H, Ris ethyl or'}{'sup': 1', '2', '4', '5, 'sub': 2', '3, 'Ris CFCl, Y is O, Ris CF, Ris H, Ris ethyl, or'}{'sup': 1', '6', '2', '4', '5', '6, 'sub': 2', '3', '3, 'Ris CFCl, Y is NR, Ris CCl, Ris H, Rand Rare CHor'}{'sup': 1', '6', '2', '4', '5', '6, 'sub': 2', '3', '3, 'Ris CFCl, Y is NR, Ris CF, Ris H, Rand Rare CHor'}{'sup': 1', '6', '2', '4', '5', '6, 'sub': 2', '3', '3, 'Ris CFH, Y is NR, Ris CCl, Ris H, Rand Rare CHor'}{'sup': 1', '6', '2', '4', '5', '6, 'sub': 2', '3', '3, 'Ris CFH, Y is NR, Ris CF, Ris H, Rand Rare CHor'}{'sup': 1', '6', '2', '4', '5', '6, 'sub': 2', '3', '3, 'Ris CFH, Y is NR, Ris CBr, Ris H, Rand Rare CHor'}{'sup': 1', '2', '4', '5, 'sub': 3', '3, 'Ris CF, Y is O, Ris CCl, Ris H, Ris ethyl, or'}{'sup': 1', '6', '2', '4', '5', '6, 'sub': 3', '3', '3, 'Ris CF, Y is NR, Ris CCl, Ris H, Rand Rare CHor'}{'sup': 1', '6', '2', '4', '5', '6, 'sub': 2', '3', '3, 'Ris CFCl, Y is NR, Ris CF, Ris H, Rand Rare CH.'}5. The process according to claim 4 , wherein the process is performed in the presence of at least one base.9. The process according to claim 4 , wherein the compound of formula (II) is present in the form of a ...

METHOD FOR PRODUCING NITROGEN-CONTAINING COMPOUND

Provided is an efficient and economical production method of a nitrogen-containing compound. A method for producing a compound represented by the formula RC(O)CH═CHNRR, including reacting a compound represented by the following formula (4) with more than 6-fold moles of a compound represented by the formula NRRC(O)H to give a reaction mixture of the compound represented by the formula () and the compound represented by the formula NRRC(O)H, and reacting the reaction mixture with a compound represented by the formula RC(O)CHby using a basic compound: 2. The method of claim 1 , wherein the reaction mixture is obtained by reacting the compound represented by formula (4) with 8- to 40-fold moles of the above mentioned compound represented by formula (3).3. The method of claim 1 , wherein the reaction mixture is mixed with a basic compound to obtain a mixture claim 1 , the mixture is mixed with the compound represented by formula (2) claim 1 , and the reaction mixture is reacted with the compound represented by formula (2).4. The method of claim 1 , wherein the reaction mixture of the compound represented by formula (4) and the compound represented by formula (3) is obtained in the presence of ether.5. The method of claim 1 , wherein the basic compound is an alkali metal alkoxide.6. The method of claim 5 , wherein the alkali metal alkoxide is a solid alkoxide of an alkali metal.7. The method of claim 5 , wherein the compound represented by formula (2) is used in an amount of more than 3-fold moles and not more than 20-fold moles relative to the compound represented by formula (4) claim 5 , and the reaction mixture is reacted with the compound represented by formula (2) in the presence of a basic compound at a reaction temperature exceeding 40° C.8. The method of claim 5 , wherein the compound represented by formula (2) is used in an amount of more than 12-fold moles relative to the compound represented by formula (4) claim 5 , and the reaction mixture is reacted with the ...

SYNTHESIS OF LEVOMETHADONE HYDROCHLORIDE OR DEXTROMETHADONE HYDROCHLORIDE AND METHODS FOR USE THEREOF

Highly efficient methods for synthesis of levomethadone hydrochloride or dextromethadone hydrochloride are provided starting from D-alanine, or L-alanine, respectively, with retention of configuration. Methods for treating a subject are provided comprising administering a composition comprising an effective amount of levomethadone hydrochloride having not more than 10 ppm dextromethadone. 1. A process for preparing levomethadone hydrochloride from D-alanine or dextromethadone hydrochloride from L-alanine , the process comprising:converting D-alanine to N,N-dimethyl-D-alaninol or converting L-alanine to N,N-dimethyl-L-alaninol;combining the N,N-dimethyl-D-alaninol or the N,N-dimethyl-L-alaninol with an activating reagent to form a R-activated intermediate or an S-activated intermediate, respectively;mixing the R- or S-activated intermediate and a base with diphenylacetonitrile to provide levomethadone nitrile or dextromethadone nitrile, respectively; andexposing the levomethadone nitrile or dextromethadone nitrile to a Grignard reagent of formula RMgX, where R is ethyl and X=Cl, Br, or I, to form a reaction mixture; andadding hydrochloric acid to the reaction mixture to provide levomethadone hydrochloride or dextromethadone hydrochloride, respectively.2. The process for preparing levomethadone hydrochloride or dextromethadone hydrochloride according to claim 1 , wherein the converting step comprises:converting the D-alanine to N,N-dimethyl-D-alanine or converting the L-alanine to N,N-dimethyl-L-alanine; andreducing the N,N-dimethyl-D-alanine to form the N,N-dimethyl-D-alaninol or reducing the N,N-dimethyl-L-alanine to form the N,N-dimethyl-L-alaninol.3. The process for preparing levomethadone hydrochloride or dextromethadone hydrochloride according to claim 1 , wherein the converting step comprises:reducing the D-alanine to form D-alaninol or reducing the L-alanine to form L-alaninol; andconverting the D-alaninol to form the N,N-dimethyl-D-alaninol or converting the ...

Method for Preparing Fluoroacylated Arylamine

A method for making fluoroacyl arylamines is disclosed. 2. (canceled)11. The method of claim 7 , comprising structure B claim 7 , wherein Y is methyl.12. The method of claim 1 , wherein said contacting comprises a solution immiscible with water.13. The method of claim 12 , wherein said solution comprises dicholoromethane.14. (canceled)15. The method of claim 1 , wherein said fluoroacyl-donating compound comprises a trifluoro anhydride or a trifluoroacetic anhydride.16. The method of claim 7 , wherein said fluoroacyl-donating compound comprises a trifluoroacetic anhydride or a trifluoro anhydride.17. The method of claim 1 , wherein said contacting occurs at a temperature from about 25° C. to about 90° C.18. The method of claim 1 , wherein said contacting occurs under reflux.19. The method of claim 1 , wherein said isolating comprises contacting said mixture with a solution comprising water.20. The method of claim 12 , comprising isolating said fluoroacyl arylamine from said solution immiscible with water.21. The method of claim 7 , wherein said contacting comprises a solution immiscible with water claim 7 , wherein the solution optionally comprises dicholoromethane.22. The method of claim 7 , wherein said contacting occurs at a temperature from about 25° C. to about 90° C. claim 7 , wherein said contacting optionally occurs under reflux. A novel method for synthesizing fluoroacylated arylamines is provided. The method is undemanding with good product yield. The compounds have favorable electroactivity and are suitable for organic electronic applications.Arylamines are used in organic electronics applications including use in photoreceptors, thin film transistors (TFT), photovoltaic (PV) cells, light emitting diodes (LEDs) etc. In the electrophotographic imaging field, the photoactive portions of components can be composed of organic materials, such as, the fluoacylated arylamines of interest, which act as photoreceptors for temporarily forming an image in the form of ...

METHOD FOR PREPARING AN N-CYCLOPROPYLMETHYL ANILINE COMPOUND

Provided is a method for preparing an N-cyclopropylmethyl aniline compound, which comprises hydrogenating a compound represented by Formula II and cyclopropyl formaldehyde as raw materials in the presence of an acid and catalyst to generate an N-cyclopropylmethyl aniline compound represented by Formula I, wherein R is alkoxy, alkylamino or a substituted anilino group represented by Formula III. 3. The method according to claim 1 , wherein the hydrogenation is carried out in a solvent which is any one or a combination of at least two selected from the group consisting of an alcohol solvent claim 1 , an ester solvent claim 1 , an ether solvent claim 1 , a halogenated hydrocarbon solvent or a benzene solvent.4. The method according to claim 3 , wherein the alcohol solvent includes any one or a combination of at least two selected from the group consisting of methanol claim 3 , ethanol and isopropanol.5. The method according to claim 1 , wherein the acid includes inorganic acids or organic acids.6. The method according to claim 1 , wherein the catalyst includes any one of palladium carbon claim 1 , platinum carbon or Raney nickel.7. The method according to claim 1 , wherein the molar ratio of the compound represented by Formula II to cyclopropyl formaldehyde is 1:(0.5-3).8. The method according to claim 1 , wherein the hydrogenation reaction is carried at a temperature of 30-150° C. claim 1 , for 8-20 h.9. The method according to claim 1 , wherein the pressure of the hydrogenation reaction after introducing hydrogen gas is controlled to be 0.2-5.0 MPa.11. The method of wherein the alkoxy group is selected from methoxy claim 2 , ethoxy claim 2 , propoxy or isopropoxy.12. The method of wherein the alkylamino group is a methylamino group.13. The method according to wherein the ester solvent includes any one or a combination of at least two selected from the group consisting of methyl acetate claim 4 , ethyl acetate claim 4 , propyl acetate and butyl acetate.14. The method ...

METHOD FOR PRODUCING RING-HALOGENATED N,N-DIALKYLBENZYLAMINES

The invention relates to a method for preparing ring-halogenated N,N-dialkylbenzylamines and intermediates obtainable therefrom for preparing agrochemicals and pharmaceutically active ingredients. 2. The method as claimed in claim 1 , characterized in that 2-chloro-N claim 1 ,N-dimethylhenzylamine is prepared by reacting 2-chlorobenzyl chloride with dimethylamine.3. The method as claimed in or claim 1 , characterized in that the reaction temperature is between 50 and 200° C. claim 1 , preferably between 90 and 180° C. claim 1 , especially preferably 130 to 150° C.4. The method as claimed in any of to claim 1 , characterized in that the reaction pressure is 2 to 300 bar claim 1 , preferably 4 to 50 bar and particularly preferably 5 to 35 bar.5. The method as claimed in any of to claim 1 , characterized in that said method is carried out continuously.7. The method as claimed in claim 6 , characterized in that 2-chloro-N claim 6 ,N-dimethylbenzylamine is used containing 2-chlorobenzaldehyde.8. The method as claimed in or claim 6 , characterized in that sodium borohydride is used.9. The method as claimed in any of to claim 6 , characterized in that said method was carried out subsequent to a method as claimed in to .109. The use of compounds of the formula (I) claims 1 , which were prepared as claimed in any of to claims 1 , in metalation reactions.11. The use as claimed in claim 10 , characterized in that the metalation reaction is a Grignard reaction. The invention relates to a method for preparing ring-halogenated N,N-dialkylbenzylamines and intermediates obtainable therefrom for preparing agrochemicals and pharmaceutically active ingredients.Ring-halogenated N,N-dialkylbenzylamines are useful intermediates in methods for preparing agrochemicals and pharmaceutically active ingredients, since they enable, by metalation, such as lithiation or conversion to Grignard reagents, a further substitution on the aromatic ring by reaction, for example, with oxalic esters.JP ...

CRYSTAL FORMS AND METHODS OF SYNTHESIS OF (2R, 6R)-HYDROXYNORKETAMINE AND (2S, 6S)-HYDROXYNORKETAMINE

The disclosure provides a method for synthesizing free base forms of (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine. In an embodiment synthesis of (2R,6R)-hydroxynorketamine (HNK) includes preparation of (R)-norketamine via chiral resolution from racemic norketamine via a chiral resolution with L-pyroglutamic acid. The disclosure also provided crystal forms of the corresponding (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine hydrochloride salts. 2. The crystalline form of claim 1 , wherein the crystalline form contains no detectable amounts of other hydroxynorketamine or hydroxynorketamine salts crystalline forms as determined by x-ray powder diffraction.34-. (canceled)5. A method for the chiral resolution of norketamine claim 1 , comprisingadding (D)-(R)-pyroglutamic acid to racemic norketamine in a solvent, forming solid (S)-norketamine D-pyroglutamate and converting the (S)-norketamine D-pyroglutamate to (S)-norketamine; oradding (L)-(S)-pyroglutamic acid to racemic norketamine in a solvent, forming solid (R)-norketamine L-pyroglutamate, and converting (R)-norketamine L-pyroglutamate to (R)-norketamine.67-. (canceled)9. The method according to claim 8 , wherein Ris tert-butyl and wherein cleaving the carbamate linkage comprises treatment of the compound of Formula IIa or Formula IIb with acid.10. The method according to claim 9 , wherein the acid is trifluoroacetic acid.11. The method according to claim 8 , additionally comprising treating (2R claim 8 ,6R)-hydroxynorketamine with hydrochloric acid to manufacture (2R claim 8 ,6R)-hydroxynorketamine hydrochloride salt claim 8 , or treating (2S claim 8 ,6S)-hydroxynorketamine with hydrochloric acid to manufacture (2S claim 8 ,6S)-hydroxynorketamine hydrochloride salt.12. (canceled)13. The method according to claim claim 8 , wherein the base is a strong base which is lithium diisopropylamide claim 8 , sodium hexamethyldisilazane claim 8 , potassium hexamethyldisilazane claim 8 , or ...

HIGHLY ENANTIOSELECTIVE ACCESS TO CYCLIC BETA-AMINO ACIDS

Disclosed herein is a method of forming a compound of formula I: 2. The method according to claim 1 , wherein Rand Reach independently represent ROC(O)— claim 1 , Cto Calkyl claim 1 , phenyl claim 1 , and naphthyl claim 1 , where the Cto Calkyl claim 1 , phenyl claim 1 , and naphthyl are unsubstituted or substituted by one or more substituents selected from the group consisting of halo and Cto Calkyl claim 1 , which Cto Calkyl is unsubstituted or substituted by one or more halo groups.3. The method according to claim 1 , wherein Rrepresents H claim 1 , Cto Calkyl claim 1 , and phenyl claim 1 , where the Cto Calkyl and phenyl are unsubstituted or substituted by one or more substituents selected from the group consisting of halo and Cto Calkyl claim 1 , which Cto Calkyl is unsubstituted or substituted by one or more halo groups.4. The method according to claim 1 , wherein Rrepresents Cto Calkyl claim 1 , Cto Calkenyl claim 1 , phenyl claim 1 , naphthyl and furanyl claim 1 , where the Cto Calkyl claim 1 , Cto Calkenyl claim 1 , phenyl claim 1 , naphthyl and furanyl are unsubstituted or substituted by one or more substituents selected from the group consisting of halo claim 1 , phenyl claim 1 , OCto Calkyl and Cto Calkyl claim 1 , which phenyl claim 1 , OCto Calkyl and Cto Calkyl are unsubstituted or substituted by one or more halo groups.5. The method according to claim 1 , wherein Ris selected from a tosyl group claim 1 , a nosyl group claim 1 , and a diphenylphosphinyl group and suitable isomers thereof.6. The method according to claim 1 , wherein Rand Rand Rto Rare each independently Cto Calkyl that is unsubstituted or substituted by one or more halo groups.8. The method according to claim 1 , wherein the base further comprises a further base selected from one or more of the group consisting of KHPO claim 1 , an amine base claim 1 , and NaHPO.9. The method according to claim 8 , wherein the amine base is selected from one or more of the group consisting of EtN claim ...

CONTINUOUS TWO STEP FLOW SYNTHESIS OF M-AMINO ACETOPHENONE

Disclosed herein is a continuous tubular reactor based conversion of acetophenones to amino substituted acetophenones wherein the nitration is carried out at −10 to 10° C. followed by reduction to m-nitrophenone resulting in uniform output of product, said process comprising the steps of: a) Nitrating acetophenone with nitrating agent (nitration mixture or fuming nitric acid) at −10 to 10° C.; b) Isolating m-nitro acetophenone from a mixture of o and m-nitro acetophenone and c) Reducing the m-nitro to obtain m-amino acetophenone. 1. A continuous method of conversion of acetophenones to amino substituted acetophenones using tubular reactor wherein the nitration is carried out at 0-10° C. followed by reduction to m-nitrophenone resulting in uniform output of product , said process comprising the steps of:a) nitration of acetophenone with nitration mixture at 0-10° C. or with fuming nitric acid at −10-20° C.;b) Isolating the m-nitro acetophenone from a mixture of o and m-nitro acetophenone by quenching of the reaction in ice and extraction in an organic solvent; and(c) Reduction of the m-nitro acetophenone with a reducing agent to obtain m-amino acetophenone.2. The continuous method of conversion of acetophenones to amino substituted acetophenones using tubular reactor according to claim 1 , wherein the acetophenone is dissolved in sulfuric acid prior to subjecting to nitration process.3. The continuous method of conversion of acetophenones to amino substituted acetophenones using tubular reactor according to claim 2 , wherein the ratio of acetophenone to sulfuric acid ranges from 1:0 to 1:2.5 w/v.4. The continuous method of conversion of acetophenones to amino substituted acetophenones using tubular reactor according to claim 1 , wherein the ratio of acetophenon to nitrating mixture is 1:1.66 v/v.5. The continuous method of conversion of acetophenones to amino substituted acetophenones using tubular reactor according to claim 1 , wherein reducing agent is selected ...

FORMAMIDE MONOMERS AND POLYMERS SYNTHESIZED THEREFROM

Formamide group-containing monomers and polymers made by polymerizing the monomers are provided. Also provided are methods of polymerizing the monomers and methods of synthesizing functionalized polymers by pre- and/or post-polymerization functionalization. The monomers are non-toxic and can generate highly reactive isocyanate and isonitrile precursors in a one-pot synthesis that enables the incorporation of complex functionalities into the side-chain of the polymers that are synthesized from the monomers.

Enantioselective Syntheses of Heteroyohimbine Natural Product Intermediates

Enantioselective syntheses of cis- and trans-bicyclic dihydropyran compounds, and other intermediates, en route to heteroyohimbine alkaloids. 2. The method of wherein said amine compound is selected from pyrrolidine and (R)-1-(naphthalen-1-yl)ethanamine.3. The method of wherein said H-bond donor compound is catechol.4. The method of wherein said amine compound is (R)-1-(naphthalen-1-yl)ethanamine.5. The method of in a cyclopentyl methyl ether solvent.6. The method of wherein Ris a tosylate (Ts) protecting group.8. The method of wherein said condensation is promoted with p-toluenesulfonic acid.9. The method of wherein said acylation is achieved with methyl formate and acyl chloride.10. The method of wherein said acid catalyst is polyphosphoric acid.11. The method of wherein Ris a tosylate (Ts) protecting group.13. The method of wherein said dehydration is achieved with sodium iodide.14. The method of wherein said reprotection is achieved with magnesium metal and benzyl carbamate.15. The method of wherein said hydroboration is achieved with 9-borabicyclo[3.3.1]nonane.16. The method of wherein said acylation is achieved with sodium hydride and acyl chloride.17. The method of wherein said acid catalyst is p-toluenesulfonic acid.18. The method of wherein said benzyl carbamate protecting group is removed with hydrogenation over palladium-carbon.20. The compound of claim 19 , wherein Ris selected from tosylate (Ts) and benzyl carbamate (Cbz) protecting groups; and Ris claim 19 , independently claim 19 , methyl. This application claims priority to and the benefit of application Ser. No. 62/156,591 filed on May 4, 2015, the entirety of which is incorporated herein by reference.Alstonine (1) and serpentine (2) are pentacyclic alkaloids proposed to contain a zwitterionic indolo[2,3-a]quino-lizidine, referred to as an anhydronium base (). This structural motif is rare among natural products and is especially unusual in total synthesis, with the only examples being ...

ANTHRAQUINONE DYE USED FOR A COLOR FILTER OF A LCD

An anthraquinone compound which is suitable for forming a color filter used for a liquid crystal display device, a composition containing a resin and the anthraquinone compound, an article having a polymer layer containing the compound and a resin, a color filter containing the compound and a method for synthesis of an asymmetric anthraquinone compound are developed. 2. The compound of claim 1 , wherein at least two of Rin formula (1) are *—X-L-S1.3. The compound of or claim 1 , wherein X is oxygen atom.4. The compound of any of to claim 1 , wherein L is alkylene group having 1 to 3 carbon atoms.5. The compound of any of to claim 1 , wherein n is 2 or less and m is 2 or less.6. A composition comprising a resin and the compound of any of to .7. The composition of claim 6 , further comprises a radiation-sensitive compound.8. An article having a polymer layer formed from the composition of or .9. The article of claim 8 , wherein the polymer layer is a negative-type layer.10. A color filter comprising at least one the compound of any of to .12. The method of wherein Rof the formula (3) is aryl group and Rof the formula (4) is aryl group claim 11 , Rand Rare substituted by the group selected from the group consisting of hydroxyl group claim 11 , amino group claim 11 , thiol group claim 11 , alkyl group having 1 to 20 carbon atoms claim 11 , aryl group or combination thereof claim 11 , and the substituent of Rand the substituent of Rare different.13. A method for synthesis of an asymmetric 1 claim 11 ,4 bis(arylamine)anthraquinone compound claim 11 , comprising the steps of: {'br': None, 'sup': '1', 'sub': '2', 'Ar—NH\u2003\u2003(5)'}, '(A) reacting in the presence of boric acid a mixture of 2,3-dihydro-9,10-dihydroxy-1,4-anthraquinone and 1,4-dihydroxyanthraquinone with a compound represented by the formula (5)'}{'sup': '1', 'wherein Aris aryl group substituted by at least one group selected from the group consisting of hydroxyl group, amino group, thiol group, alkyl ...

Intermediates of unreversible hiv protease inhibitor

A compound contg. cis-epoxide of formula (II) is prepd. In the formula, R1 is aromatic radical or cycloalkyl substited lower alkyl; R2 is oxygen or single bong; P1 and P2 is selected from hydrogen, benzyloxycarbonyl, t-butoxycarbonyl and phtaloyl. The compound of formula (II) of intermediates of unreversible HIV protease inhibitor is useful for the prodn. of AIDS treating agent.

一种β-氨基酮类化合物的合成方法

一种合成β‑氨基酮类化合物的方法，所述方法为：将底物(I)、光敏剂、N,N‑二甲苯胺类化合物(II)、碱性物质、溶剂混合，在蓝色LED光照、温度15～40℃、惰性气体保护的条件下反应5～10h，之后反应液经后处理，得到β‑氨基酮类化合物(III)；本发明安全环保，不产生废气，操作危险性低；底物适应性好，各种取代基都可以实现双官能化；反应条件温和；同时，该反应具有一定的创新性，采用光催化的方式来替代传统加热的模式，减少了能耗，更加符合现代绿色化学的理念；

The method that the dibromo benzaldehyde of 2 amino 3,5 is synthesized by KBr

本申请公开了一种通过溴化钾合成2‑氨基‑3,5二溴苯甲醛的方法，包括步骤:(1)、将乙醇、水、邻硝基苯甲醛搅拌混合，升温至固体邻硝基苯甲醛全部溶解；(2)、加入还原铁粉，并滴加3～5滴盐酸，充分搅拌并继续升温至反应体系达到回流温度，保持搅拌反应；(3)、将反应液进行抽滤，向所得滤液中搅拌滴加溴素、溴化钾和水的混合液，滴加完成后，保持温度并搅拌反应；(4)、向反应液中加入过量的饱和碳酸氢钠溶液，充分搅拌，伴有固体析出，过滤获得2‑氨基‑3,5二溴苯甲醛。本发明反应将还原、溴化两步反应有机结合在一起，省略了得到中间产物邻氨基苯甲醛的过程，简化了工艺，减少了工作量。

The preparation method of 1- [2- hydroxyl -3- amino -5- (benzyloxy) phenyl]-ethyl ketone

本发明公开了1‑[2‑羟基‑3‑氨基‑5‑(苄氧基)苯基]‑乙酮的制备方法，步骤为：(1)将1‑[2‑羟基‑3‑硝基‑5‑(苄氧基)苯基]‑乙酮(II)溶于甲醇中，加入FeCl 3 /C，升温至70℃，滴加水合肼水溶液，滴加完毕，反应3‑10h；(2)趁热过滤，滤液减压浓缩至干得固体，加入蒸馏水，调节pH＝3‑4，使固体溶解；(3)调节pH＝8‑9，静置，有晶体析出，过滤得到固体为1‑[2‑羟基‑3‑氨基‑5‑(苄氧基)苯基]‑乙酮(I)；本发明的方法，产品收率90％以上、纯度≥98％，其设备要求低，安全系数高，操作简易，生产成本低，既提高产品纯度和收率，又减少了环境污染。

Synthetic method of 3, 4-diamino-benzophenone

本发明公开了一种甲苯咪唑中间体3,4‑二氨基‑二苯甲酮的合成方法，通过严格控制氨化工艺参数和加氢工艺参数，将工艺中的两个杂质：3‑氨基‑4‑羟基‑二苯甲酮和3‑氨基‑4‑氯‑二苯甲酮含量都降低到0.05%以下，保证产品质量合格的同时保证两步反应总收率达到90%，具有很高的工业化生产价值。

Ruthenium compound, raw material for forming thin film, and method for producing thin film

본 발명은, 화학기상성장법, 특히 ALD법에 이용되는 루테늄 화합물(프리커서)에 있어서, 반응성 가스와 양호한 반응성을 가지고, 증기압이 높으면서, 융점이 낮은 화합물을 제공하는 것으로, 구체적으로는, 하기 일반식(Ⅰ)로 나타내는 루테늄 화합물, 바람직하게는 일반식(Ⅰ) 중의 R 1 및 R 2 가 에틸기 또는 이소프로필기인 루테늄 화합물을 제공하는 것이다.(식 중, R 1 , R 2 및 R 3 은 각각 독립적으로 탄소수 1~5의 직쇄 또는 분기 형상의 알킬기를 나타내고, R 1 및 R 2 의 탄소수의 합은 3~10이다.) The present invention is to provide a compound having good reactivity with a reactive gas, high vapor pressure, and low melting point in a ruthenium compound (precursor) used in a chemical vapor deposition method, particularly an ALD method, specifically, To provide a ruthenium compound represented by the general formula (I), preferably a ruthenium compound in which R 1 and R 2 in the general formula (I) are an ethyl group or an isopropyl group. (wherein R 1 , R 2 and R 3 are each independently represents a linear or branched alkyl group having 1 to 5 carbon atoms, R 1 And the sum of carbon number of R 2 is 3-10.)

Method for preparing chloroketoamine using carbamate

본 발명은 구리 촉매 존재하에서 이산화탄소로 알키닐 아민을 사이클화하거나 또는 치환된 아세토아세트아미드로부터 이소시아네이트를 형성하고 가수분해하므로서 5-메틸렌 사이클릭 카바메이트를 제조하는 방법에 관한 것이다. 이들 방법에 의한 5-메틸렌 사이클릭 카바메이트는 트리클로로이소시아누릭산을 사용하여 5-(클로로메틸렌)사이클릭 카바메이트로 전환되고 가수분해에 의해 클로로케토아민으로 된다. 본 발명 방법으로부터의 클로로케토아민은 살균제로서 유용한 아미드 화합물을 형성하기 위해 추가적으로 유기산 클로라이드와 반응할 수 있다.

Method of producing 2,3-diamino-1,4-naphthoquinones

FIELD: chemistry. SUBSTANCE: invention relates to a novel method of producing 2,3-diamino-1,4-naphthoquinones of general formula given below, which can be used for producing anticancer, antiviral compounds or herbicides. 2,3-diamino-1.4-naphthoquinones correspond to general formula , where R = H, CH 3 , C 2 H 5 and other residues of saturated hydrocarbons, such as butyl and isobutyl. Method consists in that 2-(R-amino)-3-nitro-1,4-naphthoquinone is reduced in a solution consisting of ethanol, water and sodium dithionite to end products according to following scheme: . Method enables to obtain in a single step 2,3-diamino-1,4-naphthoquinone and expand range of compounds. EFFECT: wherein products are produced with higher output (up to 61–84 %). 1 cl, 5 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 607 192 C1 (51) МПК C07C 221/00 (2006.01) C07C 225/30 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ФОРМУЛА (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ 2015135962, 25.08.2015 (24) Дата начала отсчета срока действия патента: 25.08.2015 Дата регистрации: Приоритет(ы): (22) Дата подачи заявки: 25.08.2015 (45) Опубликовано: 10.01.2017 Бюл. № 1 C 1 2 6 0 7 1 9 2 Г.А. и др. Гетероциклические производные на основе замещенного 1,4-нафтохинона. IV Конденсация 2,3-диамино-1.4-нафтохинона и его монометилпроизводных с 1.3-дикетонами. Журнал органической химии, 1967, т.3, вып.1, стр. 162-168. Л.М. ГОРНОСТАЕВ и др. Синтез 2-амино(алкиламино)-3-нитро-1,4-нафтохинонов. Журнал (см. прод.) R U (54) Способ получения 2,3-диамино-1,4-нафтохинонов (57) Формула изобретения Способ получения 2,3-диамино-1,4-нафтохинонов, общей формулы Стр.: 1 C 1 (56) Список документов, цитированных в отчете о поиске: US 3084165 A, 02.04.1963. Ефимова 2 6 0 7 1 9 2 Адрес для переписки: 660049, г. Красноярск, ул. Лебедевой, 89, КГПУ им. В.П. Астафьева, научно-исследовательский отдел, Малаховой Е.В. (73) Патентообладатель(и): Федеральное государственное бюджетное образовательное ...

Process for the preparation of N-formylamine derivatives

본 발명은 의약, 농약등의 생리활성물질의 중간체 또는 기능성 고분자 물질을 합성할 수 있는 중간체로 유용한 질소에 포밀(formyl)기를 갖는 아민유도체의 새로운 제조방법으로 1차아민 또는 2차아민기를 갖는 화합물을 포름산(formic acid)과 bis(trichloromethyl)carbonate 존재 하에서 상압, 실온 부근의 온화한 조건에서 반응시킴으로써 질소(N)를 포밀(formyl)기로 보호 한 아민 유도체를 얻는 새로운 방법이다. The present invention is a novel method for preparing an amine derivative having a formyl group in nitrogen, which is useful as an intermediate for synthesizing intermediates or functional polymers of physiologically active substances such as medicines and pesticides, and compounds having primary or secondary amine groups. It is a new method to obtain an amine derivative which protects nitrogen (N) with formyl group by reacting with formic acid in the presence of bis (trichloromethyl) carbonate under normal pressure and room temperature.

Radioisotope labeled compounds for diagnosis of cancer and precursor compounds

The present invention relates to radioisotope labeled compounds for diagnosis of tumor and to precursor compounds, and more particularly, to radioisotope labeled compounds for diagnosis of tumor, which can obtain more tumor-specific positron emission tomography (PET) images with no intake of inflammatory tissues, and to precursor compounds. The radioisotope labeled compounds according to the present invention, as tyrosine derivatives, intake no inflammatory tissues so that tumor-specific PET images can be obtained. More specifically, the labeling compound according to the present invention has superior in-vivo pharmacokinetic properties to obtain a clear tumor image, and thus can be used as a PET radiopharmaceutical for diagnosis of a tumor.

Sphingosine precursor, its synthetic method, and sythetic method for sphingosine derivative using the precursor

본 발명은 스핑고신 전구체 화합물, 그 제조방법 및 이를 이용한 스핑고신 유도체의 제조방법에 관한 것으로서, 본 발명에서는 스핑고신 전구체인 [화학식Ⅰ] 화합물의 카르보닐기를 입체선택적으로 환원반응시키고 경우에 따라 이중결합을 환원시키는 단계를 더 포함하는 것을 특징으로 하는 [화학식Ⅱ]로 표시되는 광학적으로 순수한 스핑고신 유도체의 제조 방법이 제공된다. The present invention relates to a sphingosine precursor compound, a method for preparing the same, and a method for preparing a sphingosine derivative using the same. In the present invention, the carbonyl group of the compound [Formula I], which is a sphingosine precursor, is stereoselectively reduced and double-bonded as necessary There is provided a method for producing an optically pure sphingosine derivative represented by [Formula II], further comprising the step of reducing the compound. [화학식Ⅰ] [Formula I] [화학식Ⅱ] [Formula II] 여기서, X는 OH 또는 SH이고; Y는 존재하거나 존재하지 않을 수 있는데, 존재하는 경우에는 R 4 가 수소인 것을 조건으로 하여 Y가 아민기와 염을 형성할 수 있는 산이고; Z는 단일결합 또는 이중결합이고; R 1 은 수소 또는 C 1 ~ C 6 의 저급알킬이고; R 2 는 C 10 ~ C 24 의 직쇄 또는 분지쇄 탄화수소이고; R 3 는 트리페닐메틸 또는 하기 구조식으로 표시되는 벤질유도체이며 Wherein X is OH or SH; Y may or may not be present, where present, an acid capable of forming a salt with an amine group provided that R 4 is hydrogen; Z is a single bond or a double bond; R 1 is hydrogen or lower alkyl of C 1 to C 6 ; R 2 is a C 10 to C 24 straight or branched chain hydrocarbon; R 3 is triphenylmethyl or benzyl derivative represented by the following structural formula (여기서, P 및 Q는 각각 전자흡인기(electron withdrawing group)로서 P 또는 Q중 적어도 하나가 치환되어 있음); R 4 는 수소 또는 하기 구조를 갖는 에스테르 유도체임. Wherein P and Q are each electron withdrawing groups substituted with at least one of P or Q; R 4 is hydrogen or an ester derivative having the structure (여기서, R 5 는 C 1 ~ C 20 의 치환 또는 비치환된 지방족 탄화수소 또는 C 6 ~ C 30 의 치환 또는 비치환된 방향족 탄화수소임) Wherein R 5 is C 1 to C 20 substituted or unsubstituted aliphatic hydrocarbon or C 6 to C 30 substituted or unsubstituted aromatic hydrocarbon 본 발명의 제조방법에 따르면, 바람직하지 못한 라세미화 반응이나 에피머화 반응을 전혀 발생시키지 않고 입체적 및 광학적으로 순수한 스핑고신 유도체의 두가지 서로 다른 부분입체 이성체를 제조할 수 있으며 반응의 특성상 광학적으로 순수한 화합물의 분리를 위해 ...

Preparation of [(S)-(-)-alpha-methylamino phenylketone]2.(2R,3R)-tartaric acid derivative

本发明公开了[(S)－(－)－α－甲胺基苯丙酮] 2 ·(2R，3R)－酒石酸衍生物的制备方法。将(±)－α－甲胺基苯丙酮、(R)－(+)－α－甲胺基苯丙酮或夹杂部分(S)－ (－)－α－甲胺基苯丙酮的(R)－(+)－α－甲胺基苯丙酮与(2R，3R)－酒石酸衍生物在溶剂中反应成盐，然后采用常规方法，从反应产物中收集目标产物。本发明只需控制混合溶剂的比例和总量，即可获得目标产物。本发明拆分光学收率和光学纯度较高，可直接用于(1R，2S)－(－)－麻黄碱的合成。本发明还公布了一种直接加热使(R)－(－)－α－甲胺基苯丙酮消旋的方法，不需另外加入酸或碱，即可使(R)－(－)－α－甲胺基苯丙酮消旋。

The method that the dibromo benzaldehyde of 2 amino 3,5 is synthesized by hydrogen peroxide

本申请公开了一种通过双氧水合成2‑氨基‑3,5二溴苯甲醛的方法，以还原反应产物邻氨基苯甲醛和溴素为原料，通过可提高溴素利用率的双氧水，制备合成2‑氨基‑3,5二溴苯甲醛。本发明通过可提高溴素利用率的双氧水添加剂合成2‑氨基‑3,5二溴苯甲醛，收率高，且绿色无污染。

Patent DE3347867C2

Purification method of 2-(4'-diethylamino-2'-hydroxybenzoyl)benzoic acid hexyl ester

본 발명은 고순도 및 낮은 프탈산 디알킬 에스테르 함량을 제공하는 2-(4'-디에틸아미노-2'-히드록시벤조일)벤조산 헥실 에스테르의 정제 방법에 관한 것이다.

O-AMINO ACID AMIDE DERIVATIVES, THEIR PREPARATION, THEIR USE IN THE TREATMENT OF CONDITIONS OF THE CENTRAL NERVOUS SYSTEM AND CARDIOVASCULAR DISORDERS, AND COMPOSITIONS CONTAINING THEM

A kind of synthetic method of pharmaceutical intermediate

本发明涉及医药化学领域，特别是涉及一种药物中间体的合成方法。该方法以化合物Ⅰ为原料，在双三甲基硅基胺基锂催化剂的作用下，化合物Ⅰ经与金属有机试剂反应生成化合物Ⅱ。本发明针对目前合成路线在工业化生产中，产品生产路线长、收率较低的问题，创新性的使用双三甲基硅基胺基锂催化剂高收率的制备化合物Ⅱ，合成成本低，工艺简单，适合工业化大批量生产。

Process for the preparation of mono-substituted aminoquinones

PROCESS FOR OBTAINING ALPHA-AMINOALDEHYDES ALPHA-ETHYLENIC AND NOVEL COMPOUNDS OBTAINED BY THIS PROCESS

Procédé d'obtention d'alpha-aminoaldéhydes alpha-éthyléniques de formule générale: (CF DESSIN DANS BOPI) et nouveaux alpha-aminoaldéhydes alpha-éthyléniques obtenus par ce procédé, de formule générale: (CF DESSIN DANS BOPI) Process for obtaining alpha-aminoaldehydes alpha-ethylenic of general formula: (CF DRAWING IN BOPI) and new alpha-aminoaldehydes alpha-ethylenic obtained by this process, of general formula: (CF DRAWING IN BOPI)

PROCESS FOR OBTAINING ALPHA-ETHYLENIC ALPHA-AMINOALDEHYDES AND NOVEL COMPOUNDS OBTAINED BY THIS PROCESS.

PROCESS FOR THE PREPARATION OF N-PHENYL N '- (CYCLO) ALKYL PARAPHENYLENE DIAMINES.

Arylaminomethylenecamphor derivatives

Arylaminomethylenecamphor derivatives of the formula (1) where the C=C double bond is in the Z or E configuration, and the variables have the following meanings: R1 H, CH3, R2 H, C1-C6-alkyl, C3-C8-cycloalkyl, C2-C6-alkenyl, C3-C8-cycloalkenyl, aryl or substituted aryl, R3 H, C1-C6-alkyl, C3-C8-cycloalkyl, aryl, substituted aryl, C1-C6-alkoxy, C1-C8-acyl, Ar aryl, substituted aryl, hetaryl or substituted hetaryl, are used as sunscreen agents, especially in cosmetic and pharmaceutical formulations.

Process to chloroketoamines using carbamates

本发明涉及制备5－亚甲基环状氨基甲酸酯的方法,它或者通过在铜催化剂存在下,用二氧化碳环化炔胺,或者通过取代乙酰基乙酰胺生成异氰酸酯接着水解制得,用任何一个方法制得的5－亚甲基环状氨基甲酸酯,用三氯异氰脲酸转成5－(氯亚甲基)环状氨基甲酸酯,接着水解成氯酮胺。由本发明方法制得的氯酮胺,又可以与有机酸氯化物反应,生成作杀真菌剂的酰胺化合物。

Preparation method of methyl squarate

本发明公开了一种方酸甲胺甲酯的制备方法，包括以下步骤：1)将方酸、甲醇、原甲酸三甲酯投入到反应釜中，回流反应24h～72h，得到第一混合物；2)将第一混合物进行蒸馏，蒸出低沸点溶剂，得到第二混合物，控制温度为0～50℃，向第二混合物中滴加甲胺的甲醇溶液，滴加结束常温反应1～10h，得到第三混合物；3)将第三混合物蒸馏，降温析出方酸甲胺甲酯溶液，过滤得方酸甲胺甲酯粗品和滤液；4)将粗品中加入溶剂进行重结晶，得到方酸甲胺甲酯。本发明的方酸甲胺甲酯的制备方法，采用方酸和甲醇、甲胺醇溶液作为反应原料，通过控制反应温度和投料顺序，一步合成目标产物，节省了生产成本和时间，提高了产率，适于工业化生产。

Process for the preparation of N-phenyl-N'-[(cyclo)alkyl]paraphenylenediamines

The present invention relates to a process for the preparation of N-phenyl-N'-[(cyclo)alkyl]paraphenylenediamines from N-(4-hydroxyphenyl)aniline. More precisely, it consists of a process for the preparation of N-phenyl-N'-[(cyclo)alkyl]paraphenylenediamines and of N-phenylbenzoquinonimine, characterised in that N-(4-hydroxyphenyl)aniline and a N-phenyl-N'-[(cyclo)alkyl]cyclohexa-2,5-diene-1,4-diimine are reacted in solvent medium, the (cyclo)alkyl substituent being a linear or branched alkyl radical having 1 to 12 carbon atoms or a cycloalkyl radical having 5 to 8 carbon atoms. The most advantageous N-phenyl-N'-[(cyclo)alkyl]cyclohexa-2,5-diene-1,4-diimine is N-phenyl-N'-(1,3-dimethylbutyl)cyclohexa-2,5-diene-1,4-diimine because it leads to N-phenyl-N'-(1,3-dimethylbutyl)paraphenylenediamine, which is widely used as an antiozonising agent in natural or synthetic rubbers.

Racemic separation of ketamine

Alkylation process

Process for purifying 2-(4'-diethylamino-2'-hydroxybenzoyl)benzoic acid hexyl ester

The present invention relates to a process for purifying 2-(4'-diethylamino-2'-hydroxybenzoyl)benzoic acid hexyl ester providing a high purity and low phthalic acid dialkyl ester content.

Preparation method of ketamine

本发明提供一种氯胺酮的制备方法，将2‑邻氯苯基‑2‑叠氮基环己酮和还原剂溶于溶剂1中，加热到50‑70℃下反应10‑15h，反应结束后，将上述反应液冷却至室温，加入水回流，减压蒸馏除去四氢呋喃得粗产物，萃取、洗涤、干燥，减压浓缩，得2‑邻氯苯基‑2‑氨基环己酮；将2‑邻氯苯基‑2‑氨基环己酮、甲基化试剂、醋酸、氰基硼氢化钠置于反应容器中，加入溶剂2，室温下反应10‑15 h，反应结束后，加入饱和碳酸钠溶液，经萃取、洗涤、干燥、过滤、减压蒸馏，重结晶，得氯胺酮。本发明方法制备的氯胺酮，工业化程度高，产品的质量相对于现有技术也有很大的提高，不存在中间体杂质；工艺路线操作简单，成本低廉、条件温和。

Method for preparing 2-amino-3,5-dibromobenzaldehyde having high purity and yield

본 발명은 고순도, 고수율의 2-아미노-3,5-디브로모벤즈알데히드의 제조방법에 관한 것으로, 극성용매, 유무기 알칼리, 산화방지제 및 물로 이루어진 혼합용매하에서 하기 화학식 2의 2-아미노-3,5-디브로모벤조익하이드라자이드를 출발물질로 하고, 상기 출발물질 기준으로 케톤화합물, 산화제 및 물을 혼합하여 반응시킨 후 여과, 세척 및 용제 회수공정을 수행하여 고수율 및 고순도의 하기 화학식 1의 2-아미노-3,5-디브로모벤즈알데히드를 제조하는 방법에 관한 것이다. 본 발명에 따른 방법은 2-아미노-3,5-디브로모벤즈알데히드의 제조공정을 개선하고 부산물의 생성량을 줄이고 품질향상 및 제조경비를 절약하여 고수율 및 고순도의 2-아미노-3,5-디브로모벤즈알데히드를 제조할 수 있다. The present invention relates to a method for preparing 2-amino-3,5-dibromobenzaldehyde of high purity and high yield, wherein 2-amino- of Formula 2 is used under a mixed solvent comprising a polar solvent, an organic-inorganic alkali, an antioxidant, and water. Using 3,5-dibromobenzoic hydrazide as a starting material, and reacting by mixing a ketone compound, an oxidizing agent and water on the basis of the starting material, and performing filtration, washing, and solvent recovery process to achieve high yield and high purity. It relates to a method for preparing 2-amino-3,5-dibromobenzaldehyde of the formula (1). The method according to the present invention improves the manufacturing process of 2-amino-3,5-dibromobenzaldehyde, reduces the amount of by-products produced, improves the quality and saves manufacturing costs, thus making 2-amino-3,5- of high yield and high purity. Dibromobenzaldehyde can be prepared. 화학식 1 화학식 2 Chemical Formula 1 Chemical Formula 2

A process for the preparation of ketones

The present invention relates to the preparation of aminoalkyl p-hydroxyphenyl ketones. Certain of these ketones are well known as important intermediates in the production of compounds having pharmaceutical activity, for example octopamine or synephrine. The known Houben-Hoesch reaction is a variation of the Friedel-Crafts reaction and involves the condensation of a phenolic substrate with a nitrile in the presence of a Lewis acid catalyst to give a hydroxy-aryl ketone. It is an object of the invention to provide a new or improved process for the manufacture of aminoalkyl p-hydroxyphenyl ketones. According to the invention, there is provided a process for the preparation of an aminoalkyl p-hydroxyphenyl ketone comprising reacting phenol with a nitrile, in the presence of a Lewis acid catalyst, to cause condensation thereof, the process being characterised in that the reaction is carried out in a medium comprising a nitroalkane solvent for the reactants. A preferred but non-limiting feature of the invention is the productiqn of 2'amino-4-hydroxyacetophenones. The present invention is based on the surprising discovery that nitroalkanes are unexpectedly much better solvents for this reaction, being less toxic, giving a better yield and also ensuring a homogeneous reaction medium. The nitroalkanes may also be diluted with a halogenated hydrocarbon solvent, which acts as an inert diluent, thus reducing the amount of nitroalkane used, and making the reaction less hazardous.

Patent GR77444B

Prepare the chloro- 2-(trifluoroacetyl group of 4-) the improvement technique of anilinechloride

本发明提供一种制备4‑氯‑2‑(三氟乙酰基)苯胺盐酸盐的改进工艺，涉及化合物制备方法技术领域，本发明以N‑特戊酰基‑4‑氯‑2‑(三氟乙酰基)苯胺为原料，以异丁醇与特戊酸异丁酯为溶剂，然后滴加盐酸，再进行升温反应，最后降温结晶得到产物，异丁醇与特戊酸异丁酯混合溶剂的选择有助于提高产物收率，且生成的滤液体系中水与有机物分层，便于溶剂的回收利用，有利于降低生产成本，减少后期环保处理压力。

Heterojunction nano composite catalyst and preparation method and application thereof

本发明涉及一种异质结Cu‑Ru/Fe 3 O 4 @SiO 2 ‑DPA纳米复合催化剂及其制备方法和应用，属于纳米催化剂研究领域。本发明以正硅酸乙酯为硅源，DMP‑30为有机修饰剂，在NH 3 ·H 2 O的存在下，制备了Fe 3 O 4 @SiO 2 ；以Fe 3 O 4 @SiO 2 为载体，DPA表面官能化后，以氯化铜、氯化钌为原料，β‑酮酸为竞争吸附剂，在有机修饰剂的存在下，采用沉积沉淀法制备了Cu‑Ru/Fe 3 O 4 @SiO 2 ‑DPA纳米复合催化剂；并将上述催化剂用于催化制备1‑氨基蒽醌。本发明的纳米复合催化剂具有高活性、高选择性、优异的催化活性和稳定性，反应条件温和，避免了大量副产物的产生，提高了目标产物的选择性。

Process for the preparation of o-aminophenyl cyclo-propyl ketone

There is provided an effective method for the preparation of o-aminophenyl cyclopropyl ketone via the dehydrohalogenation of 1-(o-aminophenyl)-4-halo-1-butanone in the presence of a base and a phase transfer catalyst.

Method for preparing 3-aminocyclohexanone by reductive amination of 1, 3-cyclohexanedione

本发明公开了一种1,3‑环己二酮还原胺化制备3‑氨基环己酮的方法，以1,3‑环己二酮为起始原料，在加氢催化剂作用下，氢气和氨气气氛中，在反应溶剂中进行还原胺化反应。该制备方法的底物转化率高，目标产物的收率高，且制备工艺简单可控，后处理工艺简单，便于实现工业化生产。

Process for the preparation of bupropion hydrochloride

Bu bulus, bupropion hidroklorürün hazirlanmasi ile ilgilidir.Bupropion serbest bazi elde edebilmek için 3'-kloropropiofenon' un tersiyer-butilamin varliginda brom ile reaksiyonu ve sonra hidroklorik asit ilavesi ile bupropion hidroklorür' ün elde edilmesi tanimlanmistir. Bulusun temel özelligi tersiyer-butilamin' in solvent ve reaktan olarak kullanilmasidir. The present invention relates to the preparation of bupropion hydrochloride. In order to obtain bupropion free base, the reaction of 3'-chloropropiophenone with bromine in the presence of tertiary-butylamine and subsequent addition of hydrochloric acid have been described to obtain bupropion hydrochloride. The main feature of the invention is the use of tertiary-butylamine as solvent and reactant.

Arylaminomethylene camphor derivatives and uses thereof

Arylaminomethylene camphor derivative and its use

(57)【要約】 （修正有） 【課題】 アリールアミノメチレンショウノウ誘導体及 びその使用 【解決手段】 一般式１のアリールアミノメチレンショ ウノウ誘導体及び光線防遮剤としての、殊に化粧品及び 製剤学的調製剤中での使用。 ［Ｃ＝Ｃ二重結合はＺ又はＥ配置にあり、Ｒ １ はＨ、Ｃ Ｈ ３ 、Ｒ ２ はＨ、Ｃ １ 〜Ｃ ６ −アルキル、Ｃ ３ 〜Ｃ ８ − シクロアルキル、Ｃ ２ 〜Ｃ ６ −アルケニル、Ｃ ３ 〜Ｃ ８ −シクロアルケニル、アリール又は置換アリール、Ｒ ３ はＨ、Ｃ １ 〜Ｃ ６ −アルキル、Ｃ ３ 〜Ｃ ８ −シクロアル キル、アリール、置換アリール、Ｃ １ 〜Ｃ ６ −アルコキ シ、Ｃ １ 〜Ｃ ８ −アシル、Ａｒはアリール、置換アリー ル、ヘテロアリール又は置換ヘテロアリールを表す］

PROCEDURE FOR THE SYNTHESIS OF OMEGAAMINATED ACID DERIVATIVES (Machine-translation by Google Translate, not legally binding)

Compounds of the formula I < IMAGE > for use in treating epilepsy, depression, dyskinesias such as Parkinson's disease, muscular spasms of nervous origin, hypertension, hypotension, sleeping troubles, memory defects, and as anthelminthic and analgesic agents wherein R represents:- a linear or branched C2 to C12 alkyl radical a linear or branched C2 to C4 alkyl radical substituted by a phenyl or phenoxy nucleus which may be substituted by one or two linear or branched C1 to C4 alkyl radicals by one or two linear or branched C1 to C4 alkoxy radicals or by one or two halogen atoms a linear or branched C2 to C6 acyl radical substituted by a phenyl nucleus which may be substituted by one or two linear or branched C1 to C4 alkyl radicals by one or two linear or branched C1 to C4 alkoxy radicals or by one or two halogen atoms. R1 represents hydrogen, a linear or branched C2 to C11 acyl radical a linear or branched C2 to C6 acyl radical substituted by a phenyl nucleus which may be substituted by one or two linear or branched C1 to C4 alkyl radicals by one or two linear or branched C1 to C4 alkoxy radicals or by one or two atoms of halogen, such as fluorine, chlorine or bromine, R2 represents:- a hydroxyl group an alkoxy group R3O- in which R3 is a linear or branched C1 to C3 alkyl radical an amino group and n is 3, 4 or 5 or a pharmaceutically or veterinarily acceptable salt thereof.

Preparation of acetoacetarylamides

A process for preparing acetoacetarylamides of the formula I (see formula I) where R1 and R2 are identical or different alkyl radicals, 1 and m are each 0, 1 or 2, and n is 0 or 1, by addition of diketene to the appropriate arylamine by continuously reacting the arylamine with diketene in the presence of a mixture of water and of a (C1-C4)-alkanol at temperatures from 60°C to 100°C in the course of from 0.1 to 10 min.

Preparation of (S) - (-) -alpha-methylaminopropiophenone

本发明涉及化学领域，一种（S）‑（‑）‑α‑甲胺基苯丙酮的制备，将（±）‑α‑甲胺基苯丙酮与（2R，3R）‑（‑）‑酒石酸衍生物在添加有醇醚类溶剂中反应成盐，结晶过滤，得到（S）‑（‑）‑α‑甲胺基苯丙酮·（2R，3R）‑（‑）‑酒石酸衍生物盐，经酸化，碱化，用溶剂提取，蒸馏除去溶剂，得到产品（S）‑（‑）‑α‑甲胺基苯丙酮。

RACEMATE SEPARATION OF KETAMINE

Group 2 metal precursors for deposition of group 2 metal oxide films

본 발명은 분자의 이미노 부분 중에 알콕시 기를 혼입하고 있는 제 2족 금속 함유 폴리덴테이트 β-케토이미네이트 전구체, 및 이러한 제 2족 금속 함유 폴리덴테이트 β-케토이미네이트 전구체를 포함하는 조성물에 관한 것이다. 상기 화합물 및 조성물은 실리콘, 금속 니트라이드, 금속 옥사이드 및 다른 금속 층과 같은 기판 상에 화학적 기상 증착(CVD) 방법을 통해 금속 함유 막을 제작하는데 유용하다. The present invention relates to a composition comprising a Group 2 metal-containing polydentate β-ketoiminate precursor incorporating an alkoxy group in the imino portion of the molecule, and a composition comprising such a Group 2 metal-containing polydentate β-ketoiminate precursor. It is about. The compounds and compositions are useful for fabricating metal containing films via chemical vapor deposition (CVD) methods on substrates such as silicon, metal nitrides, metal oxides, and other metal layers.

A kind of synthetic method of 3,4- diamino-benzophenone

本发明公开了一种甲苯咪唑中间体3,4‑二氨基‑二苯甲酮的合成方法，通过严格控制氨化工艺参数和加氢工艺参数，将工艺中的两个杂质：3‑氨基‑4‑羟基‑二苯甲酮和3‑氨基‑4‑氯‑二苯甲酮含量都降低到0.05%以下，保证产品质量合格的同时保证两步反应总收率达到90%，具有很高的工业化生产价值。

Preparation of acetoacetarylamides

A process for preparing acetoacetarylamides of the formula I ##STR1## where R 1 and R 2 are identical or different alkyl radicals, l and m are each 0, 1 or 2, and is 0 or 1, by addition of diketene to the appropriate arylamine by continuously reacting the arylamine with diketene in the presence of a mixture of water and of a (C 1 -C 4 )-alkanol at temperatures from 60° C. to 100° C. in the course of from 0.1 to 10 min.

METHOD FOR PRODUCING 3-DIMETHYLAMINO-2,2-DIMETHYLPROPANAL

Arylaminomethylenecamphor derivates

Arylaminomethylene-camphor derivatives of formula (I) are new: R1 = H or Me; R2 = H, 1-6C alkyl, 3-8C cycloalkyl, 2-6C alkenyl; 3-8C cycloalkenyl or aryl (optionally substituted); R3 = H, 1-6C alkyl, 3-8C cycloalkyl, aryl (optionally substituted), 1-6C alkoxy or 1-8C acyl; and Ar = aryl or heteroaryl (both optionally substituted); NB the double bond is Z or E configuration.

Derivatives of omega-amino acids,the preparation and utilisation thereof,and the compositions containing these derivatives

Compounds of the formula I for use in treating epilepsy, depression, dyskinesias such as Parkinson's disease, muscular spasms of nervous origin, hypertension, hypotension, sleeping troubles, memory defects, and as anthelminthic and analgesic agents wherein R represents:- a linear or branched C2 to C12 alkyl radical a linear or branched C2 to C4 alkyl radical substituted by a phenyl or phenoxy nucleus which may be substituted by one or two linear or branched C1 to C4 alkyl radicals by one or two linear or branched C1 to C4 alkoxy radicals or by one or two halogen atoms a linear or branched C2 to C6 acyl radical substituted by a phenyl nucleus which may be substituted by one or two linear or branched C1 to C4 alkyl radicals by one or two linear or branched C1 to C4 alkoxy radicals or by one or two halogen atoms. R1 represents hydrogen, a linear or branched C2 to C11 acyl radical a linear or branched C2 to C6 acyl radical substituted by a phenyl nucleus which may be substituted by one or two linear or branched C1 to C4 alkyl radicals by one or two linear or branched C1 to C4 alkoxy radicals or by one or two atoms of halogen, such as fluorine, chlorine or bromine, R2 represents:- a hydroxyl group an alkoxy group R3O- in which R3 is a linear or branched C1 to C3 alkyl radical; an amino group; and n is 3, 4 or 5; or a pharmaceutically or veterinarily acceptable salt thereof.

Process for crystallising bupropion hydrochloride

Process for crystallising Bupropion hydrochloride comprising the following stages: a) Bupropion hydrochloride is dissolved in a mixture comprising methanol and a precipitating solvent for Bupropion hydrochloride; b) any insoluble residue is removed; c) the solution is distilled at atmospheric pressure until the precipitation reaction is triggered; d) the following are added: I) a precipitating solvent for Bupropion hydrochloride and II) hydrochloric acid until a pH <= 2 is obtained; e) the mass is cooled to a temperature less than 10~ C, preferably between 0 and 3~ C and the precipitate obtained is separated.

Preparation method of 1-methylamino-4-bromoanthraquinone

本发明公开了一种1‑甲氨基‑4‑溴蒽醌的制备方法，先将1‑甲氨基蒽醌加入到二氯乙烷溶剂中，进行搅拌溶解；将整个体系置于冷肼中，加入溴化氢；缓慢滴加过氧化氢，控制过程温度；转移至常温水浴锅中保温，继续进行溴代，待反应完成后，减蒸、洗涤、干燥即得；本发明以过氧化氢氧化溴化氢生成溴素的方法来改变溴素的生成方式从而控制溴代反应的进度，通过控制溴素的反应进程以达到当量反应的目的，可有效降低多溴代物的产生；以1，2‑二氯乙烷为溶剂时，溴代反应的速率较高，且过程易于控制，反应条件温和最终产品收率较高，摩尔收率高达90％；而且反应时间较短3h，而甲醇体系下约反应却需要11h；溶剂可回收套用，从而有效降低成本。

Process for preparing arylketoamines

Arylketoamines are prepared by reacting arylisonitrosoalkanones with hydrogen in the presence of a transition metal catalyst and a liquid carboxylic acid at a temperature of less than about 60° C.

DERIVATIVES OF OMEGA-AMINO ACIDS, THE PREPARATION AND USE THEREOF AND PREPARATIONS CONTAINING THESE DERIVATIVES.

Arylamine processes

A method for bisformylation an arylamine compound by reacting an arylamine compound with an alkyleneamine in a reaction mixture while refluxing an acid in the reaction mixture.

Polyureas made from aminocrotonates and enaminones

A polymer made by reacting a polyisocyanate with a compound having the formula below. R 1 is an organic group. R 2 is an aliphatic group or oxyaliphatic group. R 3 is an aliphatic group. The reaction forms urea groups from the isocyanate groups of the polyisocyanate and the NH groups of the compound.

Method of separating racemic ketanine

Process for the preparation of 1-aminoanthraquinones

A kind of synthetic method of Amiprol pharmaceutical intermediate 2 amino 5 chloro benzophenone

本发明公开了一种苯甲二氮唑药物中间体2‑氨基‑5‑氯‑二苯酮的合成方法。通过在2‑溴‑5‑氟硝基苯溶液中，将5‑氯‑3‑苯基‑苯并异噁唑(分子式2)和氯化镍粉末进行升温回流反应；然后再加入4‑氯苯乙胺溶液和乙二醇二甲醚溶液，继续回流反应,最后加入碳酸氢钠溶液、降温、脱色，过滤并浓缩滤液、再次降温、洗涤、脱水，得晶体2‑氨基‑5‑氯‑二苯酮。该合成方法相比于背景技术中的合成方法，反应时间大大缩短，同时本发明提供了一种新的合成路线，为进一步提升反应收率打下了良好的基础。

A kind of preparation method of stryphnonasal

本发明涉及一种盐酸肾上腺酮的制备方法，在利用氯乙酰儿茶酚和甲胺制备盐酸肾上腺酮的过程中，控制反应在醇溶液中进行，并选择四丁基溴化胺或四丁基碘化铵作为相转移催化剂。本发明所述的方法通过控制反应在醇溶液中进行，促进了反应的充分进行，同时加入四丁基溴化胺或四丁基碘化铵作为相转移催化剂，加快了反应速度，缩短了反应时间，减少了杂质的积累。无需精制，可以一次制备出高质量的盐酸肾上腺酮，为制备L‑肾上腺素提供了高质量的中间体。

Precursors for CVD/ALD of metal-containing films

Precursors useful for vapor phase deposition processes, e.g., CVD/ALD, to form metal-containing films on substrates. The precursors include, in one class, a central metal atom M to which is coordinated at least one ligand of formula (I): wherein: R 1 , R 2 and R 3 are each independently H or ogano moieties; and G 1 is an electron donor arm substituent that increases the coordination of the ligand to the central metal atom M; wherein when G 1 is aminoalkyl, the substituents on the amino nitrogen are not alkyl, fluoroalkyl, cycloaliphatic, or aryl, and are not connected to form a ring structure containing carbon, oxygen or nitrogen atoms. Also disclosed are ketoester, malonate and other precursors adapted for forming metal-containing films on substrates, suitable for use in the manufacture of microelectronic device products such as semiconductor devices and flat panel displays.

Derivatives of w-amino acids, the preparation and utilisation thereof; and the compositions containing these derivatives

ABSTRACT Derivatives of .omega.-amino acids of general formula : I also racemic or non-racemic mixtures thereof, optically pure isomers thereof and salts of these compounds formed with pharmaceutically utilisable acids, bases and metals, wherein R represents a linear or branched alkyl radical C2-C12, a linear or branched alkyl radical C2-C4 substituted by a phenyl or phenoxy nucleus which may be itself substituted, a linear or branched acyl radical C2-C6 substituted by a phenyl nucleus which may be itself substituted; R1 represents hydrogen, a linear or branched acyl radical C2-C11, a linear or branched acyl radical C2-C6 substituted by a phenyl nucleus which may be itself substituted; R2 is an amino group, and n is equal to 3, 4 or 5. Such derivatives can be used in the treatment of neurological, psychic or cardiovascular problems, and as anthelminthic and analgesic agents.

Derivatives of omega-amino acids,the preparation and utilisation thereof,and the compositions containing these derivatives

Method for producing nitrogen-containing compound

Treat different things alike synthesis the dibromo benzaldehyde of 2 amino 3,5 method

本申请公开了一种一锅煮合成2‑氨基‑3,5二溴苯甲醛的方法，包括步骤：(1)、将乙醇、水、邻硝基苯甲醛搅拌混合，升温至固体邻硝基苯甲醛全部溶解；(2)、加入还原铁粉，并滴加3～5滴盐酸，充分搅拌并继续升温至反应体系达到回流温度，保持搅拌反应；(3)、将反应液进行抽滤，向所得滤液中搅拌滴加溴素和30％的双氧水，滴加完成后，保持温度并搅拌反应；(4)、向反应液中加入过量的饱和碳酸氢钠溶液，充分搅拌，伴有固体析出，过滤，然后用无水硫酸钠干燥有机层，获得2‑氨基‑3,5二溴苯甲醛。本发明反应将还原、溴化两步反应有机结合在一起，省略了得到中间产物邻氨基苯甲醛的过程，简化了工艺，减少了工作量。

Pro-fragrances

The present invention relates to fragrance delivery systems which comprise: a) one or more pro-fragrances having formula (I) wherein G 1 and G 2 are methyl, or a cyclic hydrocarbyl unit derived from the isomers of ionone and/or damascone; R and R 1 are each independently C 1 -C 22 substituted or unsubstituted, branched or unbranched alkyl, C 2 -C 22 substituted or unsubstituted, branched or unbranched alkenyl, C 2 -C 20 substituted or unsubstituted, branched or unbranched hydroxyalkyl, C 7 -C 20 substituted or unsubstituted alkylenearyl, C 3 -C 20 substituted or unsubstituted cycloalkyl, alkyleneoxy, C 6 -C 20 aryl, C 5 -C 20 heteroaryl comprising one or more heteroatoms selected from the group consisting of nitrogen, oxygen, sulfur, and mixtures thereof; two of the units Y 1 , Y 2 , R or R 1 can be taken together to form one or more aromatic or non-aromatic, heterocyclic or non-heterocyclic, single rings, fused rings, bicyclo rings, spiroannulated rings, or mixtures thereof, said rings comprising from 3 to 20 carbon atoms and one or more heteroatoms selected from the group consisting of nitrogen, oxygen, sulfur, and mixtures thereof; b) one or more aldehyde releasing oxazolidine pro-fragrances; and c) the balance carriers, pro-fragrances, pro-accords, other perfume ingredients.

Process for synthesis of alpha alkyl amino aldehydes

IN THE CANADIAN PATENT & TRADEMARK OFFICE PATENT APPLICATION entitled: Process for synthesis of alpha alkyl amino aldehydes in the names of: Bertrand CASTRO Jean FEHRENTZ ABSTRACT OF THE DISCLOSURE The present invention relates to a process for the preparation of alpha alkyl amino aldehydes of formula in which R is alkyl or aralkyl possibly substituted, characterized in that N,O-dimethylhydroxylamine is reacted, in a basic medium, on a blocked amine ester of an aminoacid of formula

Process for preparing 1-amino-2-bromo-4-hydroxy-anthraquinone

The preparation method of 2- methylamino -5- chlorobenzophenones

本发明涉及一种2‑甲氨基‑5‑氯二苯甲酮的制备方法，包括下述步骤：(1)甲基化反应：以2‑氨基‑5‑氯二苯甲酮为原料，以一定浓度的硫酸为溶剂，甲醛为甲基化试剂在一定温度下反应得到甲基化反应液；(2)中和：将甲基化反应液滴加至一定浓度的氨水与有机溶剂的混合液中，滴加完成后经回流降温过滤或者分液浓缩得到2‑甲氨基‑5‑氯二苯甲酮粗品；(3)纯化：2‑甲氨基‑5‑氯二苯甲酮粗品经过醇溶剂进行纯化处理得到2‑甲氨基‑5‑氯二苯甲酮精制品。本发明工艺简单，产品后处理简便，环境污染小，制备得到的2‑甲氨基‑5‑氯二苯甲酮产品质量品质高，稳定性好，是一种适合工业化制备的方法。

Method for resolution of racemic ketamine

The synthetic method of 1,4- diamino-anthraquinone leuco compounds

本发明属于化学合成领域，具体涉及一种1,4‑二氨基蒽醌隐色体的合成方法。本发明以1,4‑二羟基蒽醌为原料，与水合肼和有机溶剂混合，在反应压力0.2～0.5Mpa，反应温度50～100℃条件下，与氨气反应3‑4h，反应结束后排出氨气，反应产物冷却结晶，过滤烘干得1,4‑二氨基蒽醌隐色体。本发明合成过程中不产生高COD、高氨氮、高盐废水，过滤母液可循环利用，降低氨消耗量，有效降低生产成本，产品高纯度、高收率，适合规模化生产。

Synthetic method

Process for cleavage of racemic ketamine

Dinitrobenzophenone solution and process for preparing an ether solution of diaminobenzophenones therefrom

NOVEL DINITROBENZOPHENONE SOLUTION AND PROCESS FOR PREPARING AN ETHER SOLUTION OF DIAMINOBENZOPHENONES THEREFROM Abstract of the Disclosure A novel ether solution of dinitrobenzophenone and a process for preparing an ether solution of diaminobenzophenone therefrom which comprises subjecting a dinitrobenzophenone dissolved in said ether solvent to hydrogenation in contact with a continuous nickel catalyst to obtain said solution of diaminobenzophenone dissolved in said ether solvent. In a specific embodi-ment said nickel catalyst is mounted on an inert support. In a still further embodiment, said diaminobenzophenone dissolved in said ether solvent, after removal of water therefrom, is reacted with an aromatic dianhydride to obtain a polyamic acid solution. The polyamic acid solution can be heated at a temperature above 100°C. to drive off water of cyclization and thereby obtain the corresponding polyimide resin.

Process for preparing a polyformyl arylamine

A process including reacting a substituted or unsubstituted arylamine or a mixture thereof with a Vilsmeier reagent in the presence of a weakly polar liquid.

Manufacturing method for derivatives of sphingosine and sphinganine

본 발명은 항암제, 항균제, 소염제, 위궤양제, 동맥경화제 및 면역억제제 등의 합성 중간체로 사용되는 스핑고신 및 스핑가닌 유도체의 새로운 제조방법을 제공한다. 본 발명에 따른 제조방법은 입체선택성이 높아 광학적 및 입체적으로 순수한 이성질체를 제조할 수 있고, 하나의 출발 물질로 다양한 입체이성질체 제조가 가능하며, 반응시간이 짧은 등의 장점이 있다. The present invention provides a novel method for preparing sphingosine and sphinginine derivatives used as synthetic intermediates such as anticancer agents, antibacterial agents, anti-inflammatory agents, gastric ulcers, arteriosclerosis agents and immunosuppressants. The preparation method according to the present invention has the advantages of high stereoselectivity, which allows the preparation of optically and stereoscopically pure isomers, the preparation of various stereoisomers with one starting material, and a short reaction time.

Preparation method of medicine intermediate 2-amino-5-chlorobenzophenone

本发明公开了医药中间体2‑氨基‑5‑氯二苯甲酮的制备工艺，其特征在于，具体为：将5‑氯‑3‑苯基‑2,1‑苯并异噁唑、四氢呋喃和催化剂混合，并于氢气环境中反应，待反应结束后过滤，去除所得滤液的溶剂即得2‑氨基‑5‑氯二苯甲酮粗品，纯化粗品。该工艺所制备的产品收率高，质量好，并且无固体废弃物和废水生成，适合工业化生产。

Preparation method of 2-amino-5-chlorobenzophenone

本发明提出了一种2‑氨基‑5‑氯二苯甲酮的制备方法，其包括：步骤S1、将5‑氯‑3‑苯基‑2,1‑苯并异噁唑与催化剂混合后，加入乙酸乙酯，搅拌至溶解，保持反应体系在氢气氛围下，控制反应压力为1‑5atm，20‑30℃下反应；步骤S2、将步骤S1所得反应液过滤后蒸馏除去溶剂，得到稠状物，向稠状物中加入结晶溶剂，加热溶解后，冷却析晶过滤后得到2‑氨基‑5‑氯二苯甲酮。本发明的制备反方相比现有技术，产物的收率更高，同时杂质更少，反应条件相对温和，适用于大规模工业化应用。

2-nitro-4-aminobenzaldehyde drug intermediates synthesis method

2-nitro-4-aminobenzaldehyde drug intermediates synthesis method Abstract 5 The present invention discloses 2-nitro-4-aminobenzaldehyde drug intermediates synthesis method, comprises the following steps: 2,4-dinitrobenzyl alcohol and potassium chloride solution are added to the reaction vessel, controlling the stirring speed, raises the temperature of the solution, potassium peroxodisulfate is added, continues to react; then cyclopropane solution is added, cobalt oxalate powder is 10 added, raises the temperature of the solution, continues to react, standing, and then reduces the temperature, sodium nitrate solution is added, the solution layers, separated from the oil layer, washed with trimethylamine solution, recrystallized in cetyl alcohol solution, dehydrated with dehydration, gets the finished product 2-nitro-4-aminobenzene formaldehyde.

Process to chloroketoamines using carbamates

The present invention relates to a process for preparing 5-methylene cyclic carbamates either by cyclization of an alkynyl amine with carbon dioxide in the presence of a copper catalyst or by forming an isocyanate from a substituted acetoacetamide followed by hydrolysis. The 5-methylene cyclic carbamates by either method are converted to 5-(chloromethylene) cyclic carbamates, using trichloroisocyanuric acid, followed by hydrolysis to a chloroketoamine. The chloroketoamine from the process of this invention additionally can be reacted with an organic acid chloride to form an amide compound which is useful as a fungicide.