专利号:EP-0901500-B1 优先权日:1996-05-03 标题:In situ preparation of nucleoside phosphoramidites and their use in synthesis of oligonucleotides 发明人:ZHANG ZHAODA; TANG JIN-YAN 权利人:AVECIA BIOTECHNOLOGY INC 摘要:The invention provides novel bifunctional phosphitylating reagents and their application in in situ preparation of 5'-protected nucleoside phosphoramidites and synthesis of oligonucleotides. Bifunctional phosphitylating reagents according to the invention react quickly with nucleosides under weakly acidic conditions. In addition, the bifunctional phosphitylating reagents according to the invention generate chemoselectively the corresponding nucleoside phosphoramidites in situ, without need to purify the nucleoside phosphoramidites before using them in oligonucleotide synthesis. Finally, the bifunctional phosphitylating reagents according to the invention are relatively stable and easy to handle.
专利号:US-4937367-A 优先权日:1987-07-15 标 题:Process for the preparation of intermediates for the synthesis of fosfomycin 发明人:CASTALDI GRAZIANO; GIORDANO CLAUDIO 权利人:ZAMBON SPA 摘要:A process is described for the preparation of intermediates useful in the synthesis of Fosfomycin. n More particularly, an enantioselective process is described for the preparation of derivatives of (1S,2S)-1,2-dihydroxypropyl-phosphonic acid of formula ##STR1## wherein R 2 and R 3 have the meanings reported in the specification.
专利号:US-2004203036-A1 优先权日:2001-07-09 标 题 :Multimer polynucleotide synthesis 发明人:STENGELE KLAUS-PETER; PFLEIDERER WOLFGANG 摘要:The present invention relates to a process for the preparation of polynucleotides, whereby under suitable usual conditions the free 5′-hydroxy group, whose terminal 3′-hydroxy group contains a usual protecting group, is reacted with a hydroxy group, derivatized in a previous reaction step to a phosphite amidoester, phosphpotriester or phosphonic acid ester, whereby said hydroxy group is a 3′-hydroxy function of a free or solid phase bound polynucleotide, or a solid phase bound hydroxy function. n Further the present invention relates to a kit for performing a process according to the invention, which contains at least one or more selected oligonucleotides, having a free 5′-hydroxy group and a protected 3′-hydroxy group. Further on, the present invention relates to new oligonucleotides and their use as building blocks for the synthesis of polynucleotides in the process according to the invention. n Furthermore the present invention relates to the use of the process according to the invention or the use of the kits for the preparation of poly/oligonucleotides resp. polynucleotide libraries or nucleic acid chips.
专利号:US-4033949-A 优先权日:1976-04-14 标 题:Analogs of thromboxane B2 and processes for their synthesis 发明人:KELLY ROBERT C; NELSON NORMAN A 权利人:UPJOHN CO 摘要:The present specification provides novel intermediates and novel processes for the synthesis of various side chain and skeletal analogs of Thromboxane B 2 (11β-homo-11a-oxa-PGF 2 .sub.α). These analogs are particularly and especially useful as reproductive cycle control agents.
专利号:WO-0078725-A1 优先权日:1999-06-18 标题 :Synthesis of substituted amidines 发明人:CHOUEIRY DANIELE; GIRAUD DANIEL LIONEL; SCHOTTEN THEO 权利人:LILLY CO ELI; CHOUEIRY DANIELE; GIRAUD DANIEL LIONEL; SCHOTTEN THEO 摘要:The present invention provides a process for preparing amidines starting from carboxylic acid derivatives, in which the carboxylic acid containing moiety is attached to a sp3-, or sp?2- or sp1¿-hybridized carbon atom. The sp2-hybridized carbon atom, to which the carboxylic acid containing moiety is attached to may be part of an aromatic or heteroaromatic or olefinic system.
专利号:US-7102032-B2 优先权日:2003-04-24 标 题 :Purification of amide compound 发明人:SAKANO YASUNORI; KOIKE NORIYUKI 权利人:SHINETSU CHEMICAL CO 摘要:In the synthesis of an amide compound through reaction of an acyl fluoride group-bearing compound with an amino compound, a reaction mixture contains the amide compound and hydrogen fluoride or a hydrofluoric acid amine salt. The amide compound is recovered in high purity form by adding an oxide, carbonate or hydroxide of an alkaline earth metal to the reaction mixture to convert the hydrogen fluoride or hydrofluoric acid amine salt to an alkaline earth metal fluoride salt that can be readily removed by filtration.
[参考文献]: Said Kinani, Et Al. Study Of The Chemical Derivatization Of Zearalenone And Its Metabolites For Gas Chromatography-Mass Spectrometry Analysis Of Environmental Samples. J Chromatogr A. 2008 May 9;1190(1-2):307-15.
合成参考文献
摘要:Merino, P., Science of Synthesis, (2010) 45, 14. 摘要:Ibrahim, H., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 2, 186.