合成目标产物 N-(2-Hydroxyethyl)Pyrrolidine 主要起始原料 Pyrrolidine And 2-Bromoethanol
(文献来源)合成步骤主要原料 Pyrrolidine 和 2-Bromoethanol
1-Ethoxycarbonylmethyl-Pyrrolidine-2,5-Dione置于lithium Aluminium Tetrahydride,乙醚体系中,化学反应生成N-(2-羟乙基)-吡咯烷 参考文献:Mndshojan; Kaldrikjan,Izvestiya Akademii Nauk Armyanskoi Ssr,Khimicheskie Nauki,1959,Vol. 12,P. 55 标题:Mndshojan; Kaldrikjan,Izvestiya Akademii Nauk Armyanskoi Ssr,Khimicheskie Nauki,1959,Vol. 12,P. 55
专利信息
专利号:US-10005807-B2 优先权日:2013-04-12 标题 :Synthesis of sialylated/fucosylated human milk oligosaccharides 发明人:CHASSAGNE PIERRE; KHANZHIN NIKOLAY; HEDEROS MARKUS JONDELIUS; CHAMPION ELISE; MATWIEJUK MARTIN; DEKANY GYULA 权利人:GLYCOM AS 摘要:An achemo-enzymatic synthesis of oligosaccharides of formula 1 is presented wherein R is selected from —OH, —N 3 and —OR 6 wherein R 6 is selected from allyl optionally substituted by one or more methyl, propargyl optionally substituted by one or more methyl, 2-trimethylsilyl-ethyl, —(CH 2) n —NH 2 and —(CH 2) n —N 3 wherein integer n is to 10, preferably 2 or 3, R is selected from sialyl moiety, —SO 3 H and —CH(R)—COOH wherein R is selected from H, alkyl and benzyl, R 2 is selected from H and fucosyl, R 3 is selected from H and sialyl, R 4 is selected from H and fucosyl, provided that at least one of R 3 and R 4 is H, and A is a divalent carbohydrate linker, having important biological activities and significant commercial value for the pharmaceutical and food industry.
专利号:US-8283502-B2 优先权日:2009-04-09 标题:Autocatalytic process for the synthesis of chiral propargylic alcohols 发明人:CHINKOV NICKA; WARM ALEKSANDER; CARREIRA ERICK 权利人:CHINKOV NICKA; WARM ALEKSANDER; CARREIRA ERICK; LONZA AG 摘要:An autocatalytic process for the synthesis of chiral propargylic alcohols.
专利号:WO-2014167537-A1 优先权日:2013-04-12 标题:Synthesis of sialylated/fucosylated oligosaccharides 发明人:KHANZHIN NIKOLAY; CHASSAGNE PIERRE; HEDEROS MARKUS; CHAMPION ELISE; MATWIEJUK MARTIN; DEKANY GYULA 权利人:GLYCOM AS 摘要:This invention relates to a chemo-enzymatic synthesis of oligosaccharidesof formula 1 wherein R is selected from -OH, -N 3 and -OR 6 wherein R 6 is selected from allyl optionally substituted by one or more methyl, propargyl optionally substituted by one or more methyl, 2-trimethylsilyl-ethyl, -(CH 2 ) n -NH 2 and -(CH 2 ) n -N 3 wherein integer n is to 10, preferably 2 or 3, R 1 is selected from sialyl moiety, -SO 3 H and -CH(R 5 )-COOH wherein R 5 is selected from H, alkyl and benzyl, R 2 is selected from H and fucosyl, R 3 is selected from H and sialyl, R 4 is selected from H and fucosyl, provided that one but only one of R 3 and R 4 is H, and A is selected from a bond and a divalent carbohydrate linker, having important biological activities and significant commercial value for the pharmaceutical and food industry.
专利号:US-9102966-B2 优先权日:2010-07-16 标 题:Synthesis of sialooligosaccharide derivatives 发明人:SCHROVEN ANDREAS; CHAMPION ELISE; DEKANY GYULA; RÖHRIG CHRISTOPH; VRASIDAS IOANNIS; FIGUEROA PÉREZ IGNACIO; HEDEROS MARKUS; BOUTET JULIEN; à GOSTON à GNES; KOVà CS-PÉNZES PIROSKA; Horváth Ferenc; RISINGER CHRISTIAN; PIPA GERGELY; DEMKÓ Sà NDOR; KRÖGER LARS 权利人:SCHROVEN ANDREAS; CHAMPION ELISE; DEKANY GYULA; RÖHRIG CHRISTOPH; VRASIDAS IOANNIS; FIGUEROA PÉREZ IGNACIO; HEDEROS MARKUS; BOUTET JULIEN; à GOSTON à GNES; KOVà CS-PÉNZES PIROSKA; Horváth Ferenc; RISINGER CHRISTIAN; PIPA GERGELY; DEMKÓ Sà NDOR; KRÖGER LARS; GLYCOM AS 摘要:The invention relates to a method for the synthesis of compounds of general formula (1A) and salts thereof wherein one of the R groups is an α-sialyl moiety and the other is H, X 1 represents a carbohydrate linker, A is a D-glucopyranosyl unit optionally substituted with fucosyl, R 1 is a protecting group that is removable by hydrogenolysis, the integer m is 0 or 1, by a transsialidation reaction.
专利号:US-2014228554-A1 优先权日:2011-03-18 标 题:Synthesis of new fucose-containing carbohydrate derivatives 发明人:CHAMPION ELISE; DEKANY GYULA; HEDEROS MARKUS; AGOSTON KAROLY 权利人:GLYCOM AS; GLYCOM AS 摘要:A method for the synthesis of a fucooligosaccharide glycosides by reacting a fucosyl donor with H-A-R 1 or a salt thereof, wherein A and R 1 are as defined herein, under the catalysis of an enzyme capable of transferring fucose is provided. The fucooligosaccharid glycoside compounds, or derivatives thereof, their use in the manufacture of human milk oligosaccharides, and a method of manufacture of human milk oligosaccharides, are also provided.
专利号:US-9359327-B2 优先权日:2008-06-30 标题:Process for the preparation of substituted pyrimidine derivatives 发明人:CESCO-CANCIAN SERGIO; CHEN HONGFENG; GRIMM JEFFREY S; MANI NEELAKANDHA S; MAPES CHRISTOPHER M; PALMER DAVID C; PIPPEL DANIEL J; SORGI KIRK L; XIAO TONG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H 4 receptor modulators, and to intermediates in H4 modulator synthesis.
[参考文献]: Adamo Fini, Et Al. Diclofenac Salts, Viii. Effect Of The Counterions On The Permeation Through Porcine Membrane From Aqueous Saturated Solutions. Pharmaceutics. 2012 Sep 12;4(3):413-29. [参考文献]: Joseph Gimbel, Et Al. Effectiveness And Safety Of Diclofenac Epolamine Topical Patch 1.3% For The Treatment Of Acute Pain Due To Back Strain: An Open-Label, Uncontrolled Study. Phys Sportsmed. 2011 Feb;39(1):11-8.
合成参考文献
参考文献:10.1177/009286151104500106 摘要:Zuckerman R, Getz K, Kaitin K. A New Mechanism for Tracking Publicly Available Study Volunteer Demographics. Therapeutic Innovation & Regulatory Science. 2011 Jan;45(1):55–64. doi: 10.1177/009286151104500106.