DEUTERIUM-ENRICHED BUPROPION

The present application describes deuterium-enriched bupropion, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. 2. The compound of claim 1 , wherein the compound is a compound of Formula I.5. The compound of claim 1 , wherein the compound is a compound of Formula II.8. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.9. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.10. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.11. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.12. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.13. A method of treating depression claim 1 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to treat the depression.14. A method of treating depression claim 2 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to treat the depression.15. A method of treating depression claim 3 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to treat the depression.16. A method of treating depression claim 5 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to treat the depression.17. A method of treating depression claim 6 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to treat the depression.18. A method of treating a patient in need of smoking cessation claim 1 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to ameliorate smoking by the patient.19. A method of treating a patient in need of smoking cessation claim 2 , comprising administering ...

USE OF ANTHRANILIC ACID DERIVATIVE AS MATRIX FOR MALDI MASS SPECTROMETRY

A use of an anthranilic acid derivative as a matrix for a MALDI Mass spectrometry, comprising: 2. The use of claim 1 , wherein X is hydrogen claim 1 , and Y is hydrogen or an acetyl group.3. The use of claim 1 , wherein X is a hydroxyl group and Y is a methyl group.4. The use of claim 1 , wherein the analyte comprises lipids or proteins.5. The use of claim 1 , wherein the step of applying the matrix compound and the analyte onto the sample holder further comprises:mixing the matrix compound with a solvent to form a matrix solution;mixing the matrix solution with the analyte to form a sample mixture; andapplying the sample mixture onto the sample holder.6. The use of claim 5 , wherein the solvent comprises acetonitrile and water.7. The use of claim 5 , wherein in the step of mixing the matrix solution with the analyte claim 5 , the matrix solution and the analyte are mixed in a ratio of 0.5 to 1.5:1 by volume.8. The use of claim 1 , wherein the step of applying the matrix compound and the analyte onto the sample holder further comprises:depositing the analyte onto the sample holder; anddepositing the matrix compound onto the sample holder.9. The use of claim 8 , wherein the analyte comprises biological tissues.10. The use of claim 8 , wherein the matrix compound is deposited onto the sample holder by an evaporation deposition process.11. The use of claim 1 , wherein the step of analyzing the analyte by the MALDI mass spectrometer comprising performing at least one of a MALDI-TOF mass analyzing procedure and a MALDI-TOF mass spectrometry imaging analyzing procedure.12. The use of claim 1 , wherein the step of analyzing the analyte by the MALDI mass spectrometer is performed in both positive ion mode and ion negative mode.13. The use of claim 12 , wherein the positive ion mode has a detector gain of 1800V to 2050 V claim 12 , and the negative ion mode has a detector gain of 1800V to 2050 V.14. The use of claim 1 , wherein the MALDI mass spectrometer includes a Nd:YAG ...

FLUORESCENT PROBE SENSING TYROSINE KINASE AND USE THEREOF

A fluorescent probe for detecting a tyrosine kinase using a compound having an ortho-hydroxy-benzaldehyde structure, and use thereof are provided. The fluorescent probe can show a change in fluorescence when the compound binds with a tyrosine kinase. The compound can be readily synthesized and has high stability and low cytotoxicity in vivo. The fluorescent probe can be used to image cells or tissues overexpressing the tyrosine kinase, the fluorescent probe can be effectively used in a composition for imaging the tissues and a method of imaging the tissues. Also, the fluorescent probe can be used to image cancer cells or tissues since the fluorescent probe can exhibit fluorescence when the fluorescent probe binds to the cancer cells or tissues overexpressing the tyrosine kinase. 2. The fluorescent probe of claim 1 , wherein the compound has an ortho-hydroxy-benzaldehyde structure.3. The fluorescent probe of claim 1 , wherein the compound exhibits fluorescence when the compound binds to a tyrosine kinase to break an intramolecular hydrogen bond in the ortho-hydroxy-benzaldehyde structure.4. The fluorescent probe of claim 1 , wherein the tyrosine kinase is selected from the group consisting of ABL1 (T315I) claim 1 , BRAF claim 1 , PDGFRa claim 1 , RSK2 claim 1 , TYK2 claim 1 , and Src.5. A method of screening a tyrosine kinase inhibitor using the fluorescent probe defined in .6. A method of measuring tyrosine kinase activities using the fluorescent probe defined in .7. A method of single-photon or two-photon imaging cells using the fluorescent probe defined in .8. A composition for screening a drug inhibiting overexpression of a tyrosine kinase claim 1 , comprising the fluorescent probe defined in .9. A composition for imaging cells or tissues overexpressing a tyrosine kinase claim 1 , comprising the fluorescent probe defined in .10. The composition of claim 9 , wherein the cells or tissues overexpressing the tyrosine kinase are cancer cells claim 9 , or cancer ...

Aldehydes containing hydroxyl groups

Process for preparation of 2-amino-3,5-dibromobenzaldehyde

본 발명은 하기 식(Ⅰ)로 표시되는 2-아미노-3, 5-디브로모 벤즈알데히드를 공업적으로 용이하게 제조할 수 있는 방법에 관한 것으로, 좀더 상세하게는 2개의 히드록시기를 갖는 탄소수 C 2 ∼C 4 의 글리콜, 탄소수 C 1 ∼C 4 의 알코올 및 물로 이루어진 군으로 부터 선택된 둘 또는 그 이상의 혼합용매 존재하에서 하기 식(Ⅱ)로 표시되는 벤즈하이드라자이드 화합물과 탄산염 및 수산화염을 60∼90℃의 온도범위에서 1∼15시간 동안 반응시켜 하기 식(Ⅰ)로 표시되는 2-아미노-3, 5-디브로모 벤즈알데히드를 제조하는 방법에 관한 것이다. The present invention relates to a method that can be easily produced industrially 2-amino-3, 5-dibromo benzaldehyde represented by the following formula (I), more specifically, to a carbon number having two hydroxyl groups C 2 of ~C 4 glycols, high-benzamide represented by the following formula (ⅱ) under two or more mixed solvents selected from the presence of alcohol and water in the group consisting of carbon atoms C 1 ~C 4 dryer Zaid 60~ the compound and the carbonate and hydroxyl flame It relates to a method for producing 2-amino-3, 5-dibromo benzaldehyde represented by the following formula (I) by reacting for 1 to 15 hours at a temperature range of 90 ° C.

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.

Alpha- (dialkoylamino) trifluoromethylpropiophenones.

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

Compounds for treating nervous system diseases

本发明属于医药技术领域，具有式I结构的化合物及其药学上可接受的盐，

Method for producing substituted phenylethanolamines

Aldehydes containing hydroxl groups

The present invention relates to aldehydes of the formula (I) which contain tertiary amino groups and at least one hydroxyl group. Aldehydes of this kind can be utilized broadly. Aldehydes of particular advantage can be incorporated into a polymer, and find use as curing agents and/or catalysts. Preferably they find use in adhesives and sealants

Therapeutic compounds and preparation thereof

The invention relates to compounds of the formula <FORM:1019128/C2/1> in which R and R1 are alkyl groups of 1-5 carbon atoms. The compounds may be prepared by (1) forming a trifluoromethylpropiophenone, (2) halogenating this to form an a -halotrifluoromethylpropiophenone and (3) aminating the latter with an appropriate dialkylamine. Reaction (1) may be effected by treating a trifluoromethylphenyl magnesium halide with propionic anhydride at below 0 DEG C. in an anhydrous solvent, or alternatively by treating a trifluoromethylbenzonitrile with ethyl magnesium halide to form an intermediate ketimine, which is then hydrolysed with aqueous mineral acid. Reaction (2) is preferably affected at a temperature up to 100 DEG C. with elemental bromine or chlorine, but other halogenating agents may also be used, e.g. N-bromosuccinimide, N - bromacetamide, sulphuryl chloride or N-chlorosuccinimide. Reaction (3) may be effected at 50-125 DEG C. in the presence of a solvent, which may be an excess of the dialkylamine. The products may be converted into salts, e.g. with hydrochloric, sulphuric, phosphoric, acetic, citric or benzoic acid. Examples are given of the manufacture of the hydrochlorides of a -diethylamino-o-, -m-, and -p-trifluoromethyl - propiophenones. The products are of therapeutic value (see Division A5).ALSO:As anorexigenic agents in pharmaceutical compositions, use is made of compounds of the formula <FORM:1019128/A5-A6/1> in which R and R1 are alkyl groups of 1-5 carbon atoms (see Division C2). The compounds may be used in the form of their salts. They may be mixed with solid or liquid pharmaceutical carriers suitable for oral or suppository administration, and examples are given of the preparation of tablets containing a -diethylamino-m-(or p-)-trifluoron methylpropiophenone hydrochloride. The compounds may also be included in food supplement compositions, e.g. in vitamin compositions, or used with other therapeutically active compounds, such as ...

aldehydes containing hydroxyl groups

本发明涉及式(I)的醛，其具有叔氨基和至少一个羟基。这种醛能广泛使用。特别令人感兴趣的醛能插入到聚合物中并用作固化剂和/或催化剂。优选将其用于粘合剂和密封剂中。

Method for preparing 2-amino-3, 5-dibromo benzaldehyde

본 발명은 하기 식(Ⅰ)로 표시되는 2-아미노-3, 5-디브로모 벤즈알데히드를 공업적으로 용이하게 제조할 수 있는 방법에 관한 것으로, 좀더 상세하게는 2개의 히드록시기를 갖는 탄소수 C 2 ~C 4 의 글리콜, 탄소수 C 1 ~C 4 의 알코올 및 물로 이루어진 군으로부터 선택된 둘 또는 그 이상의 혼합용매 존재하에서 하기 식(Ⅱ)로 표시되는 벤즈하이드라자이드 화합물과 탄산염 및 수산화염을 60-90℃의 온도범위에서 1~15시간 동안 반응시켜 하기 식(Ⅰ)로 표시되는 2-아미노-3, 5-디브로모 벤즈알데히드를 제조하는 방법에 관한 것이다.

Use of anthranilic acid derivative as matrix for MALDI mass spectrometry

A use of an anthranilic acid derivative as a matrix for a MALDI Mass spectrometry, comprising:preparing a matrix compound represented by the following formula:wherein X is selected from hydrogen and a hydroxyl group, and Y is selected from hydrogen, a methyl group or an acetyl group, provided that when X is hydrogen, Y is hydrogen or an acetyl group, and when X is a hydroxyl group, Y is a methyl group;applying the matrix compound and an analyte onto a sample holder; andanalyzing the analyte by the MALDI mass spectrometer.

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

一种基于高度共轭COFs的光响应模拟氧化酶及其制备方法与应用

本发明公开了一种基于高度共轭COFs的光响应模拟氧化酶及其制备方法及应用。本发明利用1,3,5‑三[4‑氨基(1,1‑联苯‑4‑基)]苯和2,5‑二乙烯基‑1,4‑苯二甲醛合成了具优异光响应模拟氧化酶性质的TABB‑BDB COF材料，可以用于5‑160mg/L范围内的尿酸检测，满足一般情况下人血清中尿酸检测需求。本发明通过设计高度共轭的共价有机框架可以实现光的有效收集和利用，并催化有色底物2,2‑联氮‑二(3‑乙基‑苯并噻唑‑6‑磺酸)二铵盐生成具氧化性的自由基(oxABTS)与具抗氧化活性的尿酸反应，通过监测体系的颜色变化实现尿酸的高效检测。

一种基于高度共轭COFs的光响应模拟氧化酶及其制备方法与应用

本发明公开了一种基于高度共轭COFs的光响应模拟氧化酶及其制备方法及应用。本发明利用1,3,5‑三[4‑氨基(1,1‑联苯‑4‑基)]苯和2,5‑二乙烯基‑1,4‑苯二甲醛合成了具优异光响应模拟氧化酶性质的TABB‑BDB COF材料，可以用于5‑160mg/L范围内的尿酸检测，满足一般情况下人血清中尿酸检测需求。本发明通过设计高度共轭的共价有机框架可以实现光的有效收集和利用，并催化有色底物2,2‑联氮‑二(3‑乙基‑苯并噻唑‑6‑磺酸)二铵盐生成具氧化性的自由基(oxABTS)与具抗氧化活性的尿酸反应，通过监测体系的颜色变化实现尿酸的高效检测。

Verfahren zur bestimmung eines analyts mit einer primären aminogruppe und kit zur etikettierung dieses analyts

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고순도 2-아미노-3,5-디브로모 벤즈알데히드의 제조방법

본 발명은 2-아미노-3,5-디브로모 벤즈알데히드를 공업적으로 유리하게 제조 및 분리하는 방법에 관한 것으로, 좀 더 구체적으로는 에틸렌글리콜, 메탄올 및 물의 혼합용매하에서 벤즈하이드라자이드 화합물에 탄산염 및 수산화염을 혼합하고, 페놀계 산화방지제 및 탈색제를 첨가하여 50∼100℃에서 1∼15시간 동안 반응시켜 색상이 우수한 고품질의 2-아미노-3,5-디브로모 벤즈알데히드를 고순도로 제조하는 방법에 관한 것이다.

A process for the production of 1(p-hydroxyphenyl)-1-hydroxy-2-(aralkyl-amino)-propanes

Aminopropanols of the formula <FORM:0669574/IV (b)/1> (where R is an aliphatic hydrocarbon residue of 2-5 carbon atoms) are prepared by the following methods: (1) hydrogenating the ketone <FORM:0669574/IV (b)/2> or a salt thereof (R1=H or group split off during hydrogenation, e.g. benzyl) with a noble metal or nickel catalyst; in the latter case, when using a salt, 1 mol. of alkali is added either initially or after 1 mol. of hydrogen has been taken up (by elimination of R1); (2) decomposing the derivative <FORM:0669574/IV (b)/3> by hydrogenation with palladium or heating with mineral acid (when R2=benzyl) or saponification (when R2=residue of a carboxylic or sulphonic acid); (3) reacting an aralkylamine with HO-C6H4-CO.CO.CH3 (or a benzyl ether or carboxylic or sulphonic ester thereof) to give a Schiff's base or aldehyde ammonia; the product is then hydrogenated with a noble metal or nickel catalyst whereby C=N and C=O bonds are reduced and the benzyloxy group if present is converted to a hydroxy group; where an ester was used as starting material, final hydrolysis gives the free p-hydroxy group; (4) an aralkyl or aralkenyl aldehyde or ketone is condensed with <FORM:0669574/IV (b)/4> (or the corresponding R2O- compound) with simultaneous or subsequent reduction; the residue R2 if present is then eliminated as in (2); (5) suspending <FORM:0669574/IV (b)/5> in an organic solvent in which it is sparingly soluble and hydrogenating it together with an aldehyde or ketone R5-CO-R4-C6H5, where R4 and R5 are aliphatic hydrocarbon residues or R5 may be hydrogen, and the sum of the carbon atoms in R4 and R5 is 1-4. In method (1) the reduction and splitting off of R1 may occur simultaneously or successively in either order, depending on the reaction conditions. Suitable solvents for method (5) are methanol, ethanol and isopropanol, with or without water. The products may be obtained as mixtures of stereoisomers which may be separated; ...

Method for the determination of an analyte comprising a primary amino group, and kit for labeling said analyte

The invention provides a method for labeling an analyte comprising a primary amino group, the method comprising: a. a labeling process comprising reacting the analyte with a dialdehyde in the presence of a label, wherein the label bears a charge, and b. an analysis process comprising subjecting the labeled analyte to MS, preferably LC-MS-MS. Herein, preferably, the labeling process comprises reacting an analyte with a dialdehyde, wherein the dialdehyde carries a label bearing a charge, to provide a labeled analyte carrying the charge. The present invention also provides a labeling method to provide a labeled analyte carrying a charge, wherein the labeling method comprises a labeling process comprising reacting an analyte with a dialdehyde, wherein the analyte comprises a primary amino group and wherein the dialdehyde carries a label bearing the charge. The dialdehyde is preferably an aromatic dialdehyde, most preferably an aromatic 1,2- or 1,3-dicarboxaldehyde. The label preferably comprises a quaternary ammonium group and/or a quaternary phosphonium group. The present invention also provides for a kit for labeling the analyte.

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基于四苯基苯的异构共价有机框架材料及制备方法

本发明公开了基于四苯基苯的异构共价有机框架材料及制备方法，其中的一种基于四苯基苯的异构共价有机框架材料用式(III)； 本发明的基于四苯基苯的异构共价有机框架材料p‑TPB‑COF‑H和p‑TPB‑COF‑M可以由相同单体1,4‑二(4‑甲酰基苯基)‑2,5‑二(4‑氨基苯基)苯通过溶剂的调控成功构筑，为异构COFs的设计合成提供了新思路，本发明的基于四苯基苯的异构共价有机框架材料，分别用于维生素B 12 的选择性吸附和水蒸气吸附。

基于四苯基苯的异构共价有机框架材料及制备方法

本发明公开了基于四苯基苯的异构共价有机框架材料及制备方法，其中的一种基于四苯基苯的异构共价有机框架材料用式(III)； 本发明的基于四苯基苯的异构共价有机框架材料p‑TPB‑COF‑H和p‑TPB‑COF‑M可以由相同单体1,4‑二(4‑甲酰基苯基)‑2,5‑二(4‑氨基苯基)苯通过溶剂的调控成功构筑，为异构COFs的设计合成提供了新思路，本发明的基于四苯基苯的异构共价有机框架材料，分别用于维生素B 12 的选择性吸附和水蒸气吸附。

Method for the determination of an analyte comprising a primary amino group, and kit for labeling said analyte

The invention provides a method for labeling an analyte comprising a primary amino group, the method comprising: a. a labeling process comprising reacting the analyte with a dialdehyde in the presence of a label, wherein the label bears a charge, and b. an analysis process comprising subjecting the labeled analyte to MS, preferably LC-MS-MS. Herein, preferably, the labeling process comprises reacting an analyte with a dialdehyde, wherein the dialdehyde carries a label bearing a charge, to provide a labeled analyte carrying the charge. The present invention also provides a labeling method to provide a labeled analyte carrying a charge, wherein the labeling method comprises a labeling process comprising reacting an analyte with a dialdehyde, wherein the analyte comprises a primary amino group and wherein the dialdehyde carries a label bearing the charge. The dialdehyde is preferably an aromatic dialdehyde, most preferably an aromatic 1,2- or 1,3-dicarboxaldehyde. The label preferably comprises a quaternary ammonium group and/or a quaternary phosphonium group. The present invention also provides for a kit for labeling the analyte.

Method for the determination of an analyte comprising a primary amino group, and kit for labeling said analyte

The invention provides a method for labeling an analyte comprising a primary amino group, the method comprising: (a.) a labeling process comprising reacting the analyte with a dialdehyde in the presence of a label, wherein the label bears a charge, and (b.) an analysis process comprising subjecting the labeled analyte to MS, preferably LC-MS-MS. Herein, preferably, the labeling process comprises reacting an analyte with a dialdehyde, wherein the dialdehyde carries a label bearing a charge, to provide a labeled analyte carrying the charge. The present invention also pro vides a labeling method to provide a labeled analyte carrying a charge, wherein the labeling method comprises a labeling process comprising reacting an analyte with a dialdehyde, wherein the analyte comprises a primary amino group and wherein the dialdeh yde carries a label bearing the charge. The dialdehyde is preferably an aromatic dialdehyde, most preferably an aromatic 1,2- or 1,3-dicarboxaldehyde. The label preferably comprises a quaternary ammonium group and/or a quaternary phosponium group. The present invention also provides for a kit for labeling the analyte.

Method for the determination of an analyte comprising a primary amino group, and kit for labeling said analyte

The invention provides a method for labeling an analyte comprising a primary amino group, the method comprising: a. a labeling process comprising reacting the analyte with a dialdehyde in the presence of a label, wherein the label bears a charge, and b. an analysis process comprising subjecting the labeled analyte to MS, preferably LC-MS-MS. Herein, preferably, the labeling process comprises reacting an analyte with a dialdehyde, wherein the dialdehyde carries a label bearing a charge, to provide a labeled analyte carrying the charge. The present invention also provides a labeling method to provide a labeled analyte carrying a charge, wherein the labeling method comprises a labeling process comprising reacting an analyte with a dialdehyde, wherein the analyte comprises a primary amino group and wherein the dialdehyde carries a label bearing the charge. The dialdehyde is preferably an aromatic dialdehyde, most preferably an aromatic 1,2- or 1,3-dicarboxaldehyde. The label preferably comprises a quaternary ammonium group and/or a quaternary phosphonium group. The present invention also provides for a kit for labeling the analyte.

1-(4-hydroxy-3-alkoxyphenyl)-2-(1-methyl-2-phenoxyethylamino)-alkanols and derivatives and process for preparing the same

The invention comprises compounds (including the stereoisomeric forms thereof) of the general formula <FORM:0995356/C2/1> (wherein R1 is a C1-5 alkyl group and R2 is a hydrogen atom or a methyl group) and the pharmaceutically acceptable, non-toxic acid addition salts thereof, pharmaceutical preparations containing them, and their preparation by (a) reacting a compound (I) of the formula <FORM:0995356/C2/2> (wherein R3 is a hydrogen atom or a group which is replaceable by a hydrogen atom, Z is a CO or CHOH group and Y1 is an amino group or a halogen atom) with a compound of the formula <FORM:0995356/C2/3> (wherein Y2 is a Hal-CH(CH3)- group when Y1 is an amino group and a H2N-CH)CH3)-group when Y1 is a halogen atom) and, when R3 is not a hydrogen atom or Z is a CO group catalytically hydrogenating the product of the formula <FORM:0995356/C2/4> or an acid addition salt thereof, or (b) catalytically hydrogenating a mixture of phenoxyacetone and a compound (I) in which Y1 is an amino group, optionally followed in either case by acid addition salt formation. The product may be separated into individual racemates, or this separation may be effected before the catalytic hydrogenation in process (a). a - Bromo - 4 - benzyloxy - 3 - methoxypropiophenone is prepared from 4-hydroxy-3-methoxypropiophenone, via 4-benzyloxy-3-methoxypropiophenone. 4-Hydroxy-3-ethoxyacetophenone is prepared from 2-ethoxyphenol. The compounds of the invention are uterine muscle relaxants, anti-hypertensive agents and vasodilators, and may be administered orally or parenterally in the form of pharmaceutical preparations (e.g. elixirs, solutions, suspensions, tablets and capsules) containing them together with a carrier.

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Composés cétoniques de la série du diphényl méthane et leur préparation

Verfahren zur Herstellung von 1-(3',4'-Dioxy-phenyl)-2-(a-methyl-y-phenyl-propylamino)-1-oxo-propan

1-(4-hydroxy-3-alcoxyphényl)-2-(1-méthyl-2-phénoxyéthylamino)alcanols et dérivés de ces composés.

Procédé de préparation de 1-(4-hydroxy-3-alcoxyphényl)-2-(1-méthyl-2-phénoxyéthylamino) alcanols et des dérivés de ces composés, et produits obtenus

Verfahren zur Herstellung von 1-(3',4'-Dioxy-phenyl)-2-(a-methyl-y-phenyl-propylamino)-1-oxo-propan

Werkwijze voor het vervaardigen van gelaagd vloerbedekkingsmateriaal.

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Diphenyl ketones of pharmaceutical value and the preparation thereof

The invention comprises the compounds 6-ethylmethylamino-5-methyl-4, 4-diphenylhexan-3-one and 6-ethylmethylamino-4, 4-diphenylheptan-3-one, and their salts. The compounds are analgesics and may be prepared by treating 3-ethylmethylamino-2-methyl-1, 1-diphenyl-propyl cyanide or 3-ethylmethylamino-1, 1-diphenylbutyl cyanide, respectively, with ethyl magnesium bromide. In examples, ethylmethylamine is heated with propylene oxide to give 1-ethylmethylamino-2-propanol which is reacted with thionyl chloride in chloroform to yield 1-ethylmethylamino-2-chloropropane; this is then refluxed with diphenylmethyl cyanide and sodamide in benzene to produce a mixture of the isomers 3-ethylmethylamino-1, 1-diphenylbutyl cyanide and 3-ethylmethylamino-2-methyl-1, 1-diphenylpropyl cyanide. After separation, these compounds are reacted with ethyl magnesium bromide according to the Grignard process. The oxalate and the hydroiodide of 6-ethylmethylamino-5-methyl-4, 4-diphenylhexan-3-one, and the hydrobromide of 6-ethylmethylamino-4, 4-diphenylheptan-3-one are described. The Provisional Specification refers to Specifications 654,975, 677,522 and 688,481.

一种基于高度共轭COFs的光响应模拟氧化酶及其制备方法与应用

本发明公开了一种基于高度共轭COFs的光响应模拟氧化酶及其制备方法及应用。本发明利用1,3,5‑三[4‑氨基(1,1‑联苯‑4‑基)]苯和2,5‑二乙烯基‑1,4‑苯二甲醛合成了具优异光响应模拟氧化酶性质的TABB‑BDB COF材料，可以用于5‑160mg/L范围内的尿酸检测，满足一般情况下人血清中尿酸检测需求。本发明通过设计高度共轭的共价有机框架可以实现光的有效收集和利用，并催化有色底物2,2‑联氮‑二(3‑乙基‑苯并噻唑‑6‑磺酸)二铵盐生成具氧化性的自由基(oxABTS)与具抗氧化活性的尿酸反应，通过监测体系的颜色变化实现尿酸的高效检测。

基于四苯基苯的异构共价有机框架材料及制备方法

本发明公开了基于四苯基苯的异构共价有机框架材料及制备方法，其中的一种基于四苯基苯的异构共价有机框架材料用式(III)； 本发明的基于四苯基苯的异构共价有机框架材料p‑TPB‑COF‑H和p‑TPB‑COF‑M可以由相同单体1,4‑二(4‑甲酰基苯基)‑2,5‑二(4‑氨基苯基)苯通过溶剂的调控成功构筑，为异构COFs的设计合成提供了新思路，本发明的基于四苯基苯的异构共价有机框架材料，分别用于维生素B 12 的选择性吸附和水蒸气吸附。

多取代烯胺醛衍生物及其制备方法

本发明提供了一种多取代烯胺醛衍生物及其制备方法，包括：将丙烯醛或丙烯醛衍生物、叠氮化合物或叠氮衍生物、强酸和溶剂置于反应容器中，在0℃以下反应10～60min，再加入甲醇，继续反应10～120min，反应完成后加入三乙胺终止反应；将反应液用二氯甲烷稀释，再经水洗，得有机相；其中，二氯甲烷的用量是所述溶剂体积的5～10倍；将得到的有机相经干燥、浓缩和柱层析纯化，得到多取代烯胺醛衍生物；所述多取代烯胺醛衍生物的结构式如下：