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CAS号96-43-5 2-氯噻吩 | CAS号58457-24-2 5-氯-4-硝基噻酚-2-磺酰氯 | CAS号53595-66-7 5-氯噻吩-2-磺酰胺 | CAS号155731-14-9 5-氯-2-噻吩叔丁基磺酰胺 | CAS号78380-28-6 5-氯噻吩-2-磺酰肼 | CAS号83222-18-8 5-chloro-N-diaz... | CAS号620103-77-7 5-chloro-N-quin...2-氯噻吩置于磺酰氯,N,N-二甲基甲酰胺体系中,化学反应 1.0H,以60%的收率获得5-氯噻唑-2-磺酰氯
参考文献:The Use Ofn,N-Dimethylformamide-sulfonyl Chloride Complex For The Preparation Of Thiophenesulfonyl Chlorides
标题:The Use Ofn,N-Dimethylformamide-sulfonyl Chloride Complex For The Preparation Of Thiophenesulfonyl Chlorides
摘要:发现1:1的n,N-二甲基甲酰胺-so2Cl2复合物是一种有效的试剂,可用于一步法合成噻吩磺酰氯.
Doi:10.1246/bcsj.58.1063
专利信息
专利号:US-7138526-B1
优先权日:1999-06-15
标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives
发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M
权利人:AVENTIS PHARMA INC
摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:US-8440844-B2
优先权日:2011-06-21
标题 :Process for the preparation of β-amino alcohol
发明人:RAWAT VARUN; CHOUTHAIWALE PANDURANG VILASRAO; CHAVAN VILAS BHIKU; SURYAVANSHI GURUNATH MALLAPPA; SUDALAI ARUMUGAM
权利人:RAWAT VARUN; CHOUTHAIWALE PANDURANG VILASRAO; CHAVAN VILAS BHIKU; SURYAVANSHI GURUNATH MALLAPPA; SUDALAI ARUMUGAM; COUNCIL SCIENT IND RES
摘要:A high-yielding enantioselective synthesis of the bioactive (S)—N-(5-chlorothiophene-2-sulfonyl)-β,β-diethylalaniol (7.b.2), a Notch-1-sparing γ-secretase inhibitor metabolite (with EC 50 =28 nM) effective in reduction of Aβ production in vivo, has been realized starting from readily available 3-pentanone. The key steps of the synthesis are proline-catalyzed α-aminooxylation and α-amination of aldehyde; the latter contributing an overall yield of 50-75% and 90-99% enantiomeric excess.
专利号:US-9574189-B2
优先权日:2005-12-01
标题:Enzymatic encoding methods for efficient synthesis of large libraries
发明人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK
权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS
摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).
专利号:US-8138272-B2
优先权日:2006-05-22
标 题:Preparation of polymer conjugates of therapeutic, agricultural, and food additive compounds
发明人:KONRADI ANDREI W; SMITH JENIFER L
权利人:KONRADI ANDREI W; SMITH JENIFER L; ELAN PHARM INC
摘要:This invention provides an improved synthesis of polymer conjugates of formula (I), n nof agricultural, therapeutic, and food additive compounds. In particular, a process is described for the preparation of conjugates by treating primary or secondary alcohol substituents of active compounds with polymeric nucleophiles using “Mitsunobuâ€? or related reaction conditions.
专利号:US-6800764-B2
优先权日:2001-12-11
标题:Process for the synthesis of chirally pure beta-amino-alcohols
发明人:KREFT ANTHONY FRANK; ANTANE MADELENE MIYOKO; COLE DEREK CECIL; KUBRAK DENNIS MARTIN; RESNICK LYNN; STOCK JOSEPH RAYMOND; WANG ZHENG
权利人:WYETH CORP
摘要:A process is provided for preparing chirally pure S-enantiomers of alpha-amino acids comprising the steps of: a) preparing an organometallic reagent from an alkyl halide of the formula (R)2CH(CH2)nCH2X; b) adding the organometallic reagent to carbon dioxide to afford a carboxylic acid; c) activating the carboxylic acid with an acid chloride, phosphorus trichloride, acid anhydride, or thionyl chloride in the presence of a tertiary amine base; d) reacting the product of step c) with an alkali metal salt of S-4-benzyl-2-oxazolidinone; e) treating the product of step d) with a strong non-nucleophilic base to form an enolate anion; f) trapping the enolate anion with 2,4,6-triisopropylbenzenesulfonyl azide to afford an oxazolidinone azide; g) hydrolyzing the oxazolidinone azide with an aqueous base to afford an alpha-azido acid; h) reducing the alpha-azido acid to the alpha-amino acid; and i) recrystallizing the alpha-amino acid to the chirally pure alpha-amino acid. A process is also provided for preparing chirally pure S-enantiomers of beta-amino alcohols further comprising the steps of reducing the crude alpha-amino acid to the beta-amino alcohol and recrystallizing the beta-amino alcohol to the chirally pure beta-amino alcohol. A process is further provided for preparing chirally pure S enantiomers of N-sulfonyl beta-amino alcohols further comprising the steps of sulfonylating the beta-amino alcohol with 5-chloro-thiophene-2-sulfonyl halide; and recrystallizing to afford the chirally pure N-sulfonyl beta-amino alcohols.
专利号:US-9422244-B2
优先权日:2010-01-29
标 题 :Synthesis of substituted pyrazoline carboxamidine derivatives
发明人:VAN LOEVEZIJN ARNOLD; LANGE JOSEPHUS H M; BARF GERRIT A; DEN HARTOG ARNOLD P
权利人:VAN LOEVEZIJN ARNOLD; LANGE JOSEPHUS H M; BARF GERRIT A; DEN HARTOG ARNOLD P; ABBVIE BAHAMAS LTD
摘要:This invention relates to organic chemistry, in particular to processes for the preparation of pyrazoline carboxamidine derivatives of formula (I), known as potent 5-HT6 antagonists. The invention also relates to novel intermediates of these compounds. wherein the symbols have the meanings given in the description.