1-烯丙基-4-(2-羟基乙基)-哌嗪置于硫代水杨酸,1,4-双(二苯基膦)丁烷,Bis(Dibenzylideneacetone)-Palladium(0)体系中,用 四氢呋喃 用作溶剂,化学反应 0.5H,以100%的收率获得n-羟乙基哌嗪 参考文献:Selective Deprotection Of Allyl Amines Using Palladium 标题:Selective Deprotection Of Allyl Amines Using Palladium 摘要:Mono And Diallylamines Can Be Cleaved Using Pd(0) Catalyst And 2-Mercaptobenzoic Acid As Nucleophile. This Methodology Has Been Successfully Used For The Sequential Deprotection Of Diallylamines. The Yields Of Desallylation Are Good To Quantitative. Doi:10.1016/0040-4039(95)00003-U
专利号:US-6531591-B1 优先权日:1999-07-07 标 题 :Synthesis of stable quinone and photoreactive ketone phosphoramidite reagents for solid phase synthesis of photoreactive-oligomer conjugates 发明人:FENSHOLDT JEF 权利人:EXIQON AS 摘要:Quinone phosphoramidite reagents as well as photoreactive ketone phosphoramidite reagents, such as anthraquinone phosphoramidite reagents and benzophenone phosphoramidite reagents were synthesized and used for the solid phase synthesis of photoreactive-oligonucleotide conjugates. These phosphoramidite reagents are stable, suitable for large-scale synthesis and designed for automated solid phase synthesis of oligomers terminating in a photoreactive moiety.
专利号:EP-1202998-B1 优先权日:1999-07-07 标 题 :Synthesis of stable quinone and photoreactive ketone phosphoramidite reagents for solid phase synthesis of photoreactive-oligomer conjugates 发明人:FENSHOLDT JEF 权利人:EXIQON AS 摘要:Quinone phosphoramidite reagents as well as photoreactive ketone phosphoramidite reagents, such as anthraquinone phosphoramidite reagents and benzophenone phosphoramidite reagents were synthesized and used for the solid phase synthesis of photoreactive-oligonucleotide conjugates. These phosphoramidite reagents are stable, suitable for large-scale synthesis and designed for automated solid phase synthesis of oligomers terminating in a photoreactive moiety.
专利号:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
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-4709034-A 优先权日:1986-02-14 标 题 :Process for the synthesis of hydroxyalkyl amines and hydroxyalkyl piperazines 发明人:MARSELLA JOHN A 权利人:AIR PROD & CHEM 摘要:The present invention comprises a process for the synthesis of hydroxyalkyl amines, hydroxyalkyl piperazines, or alkyl piperazines from alkylene glycols and ammonia or alkyl amines using a substantially soluble transition metal carbonyl complex catalyst precursor.
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.
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