📜苯甲酰乙腈置于lithium Aluminium Tetrahydride体系中,用 四氢呋喃 作为反应溶剂,以64%的收率获得产物3-氨基-1-苯基丙烷-1-醇 参考文献:Arylpropanolamines Incorporating An Antioxidant Function As Neuroprotective Agents 标题:Arylpropanolamines Incorporating An Antioxidant Function As Neuroprotective Agents 摘要:我们合成了一系列含有二吡咯烷基嘧啶作为抗氧化功能的芳基丙醇胺,并将其评估为具有双重功能的神经保护剂.对它们作为钠通道阻断剂和抗氧化剂的体外功效进行了评估,并将其与乙醇胺衍生物(1)的体外功效进行了比较.研究表明,这些化合物能将 3H-Btx 毒素从大鼠脑膜部分的钠离子通道中置换出来,其能力在很大程度上与芳基环上的取代基无关,这表明这种活性可能主要与氨基嘧啶分子有关.抗氧化功效的结构-活性关系不太明确,但非对称嘧啶的活性始终高于其对称异构体.报告对这一观察结果进行了简要的理论研究. DOI:10.1071/ch03010
专利号:US-7160517-B2 优先权日:2000-08-18 标题 :Apparatus and methods for the automated synthesis of oligosaccharides 发明人:SEEBERGER PETER H; PLANTE OBADIAH J 权利人:MASSACHUSETTS INST OF TECHNOLG 摘要:One aspect of the present invention relates to an apparatus for the efficient synthesis of oligosaccharides on a solid support, e.g., formed by subunit addition to terminal subunits immobilized on solid-phase particles. In certain embodiments, the apparatus of the present invention is used in combinatorial methods, e.g., as described herein, of synthesizing oligosaccharides.
专利号:US-8138330-B2 优先权日:2006-09-11 标 题 :Process for the synthesis of oligonucleotides 发明人:LEUCK MICHAEL; WOLTER ANDREAS; STUMPE ALFRED 权利人:LEUCK MICHAEL; WOLTER ANDREAS; STUMPE ALFRED; SIGMA ALDRICH CO LLC 摘要:The present invention discloses novel methods for the synthesis of oligonucleotides with nucleoside phosphoramidites on solid supports. The methods comprise the stepwise chain assembly of oligonucleotides on supports with 5′-acyl phosphoramidites. The synthesis cycles consist of a front end deprotection step which is conducted with a solution of a primary amine or a phenolate, a phosphoramidite coupling step with a 5′-acyl nucleoside phosphoramidite in the presence of an activator, a phosphite oxidation step and an optional capping step. The novel methods improve the quality of synthetic oligonucleotides due to the irreversibility of the front end deprotection step, which prevents the formation of deletion sequences, and due to the avoidance of acidic reagents in the synthesis cycles, which prevent the formation of depurination side products. The invention further discloses novel nucleoside phosphoramidite compositions wherein the phosphoramidites carry acyl front end protective groups which are cleavable with primary amines or phenolates. The invention is applicable to the synthesis of oligodeoxyribonucleotides, oligoribonucleotides and oligonucleotides with modifications in their sugar or phosphate groups.
专利号:US-5541314-A 优先权日:1993-02-11 标题:Method for automated synthesis of oligonucleotides 发明人:MCGRAW ROYAL A; GROSSE WILLIAM M 权利人:UNIV GEORGIA RES FOUND 摘要:Apparatus and method for the automated synthesis of DNA segments utilizing multiple reaction columns, all of which are open at the inlet end to the atmosphere of a reaction chamber. A movable reagent supply line outlet is positioned adjacent to the column inlet end to apply reagent to each of the columns according to an input sequence of delivery. The delivery sequence is under processor control. Reagents are removed from all columns simultaneously through the application of vacuum at the outlet end of each column. The device enables the parallel synthesis of large numbers of different oligonucleotide sequences of different lengths.
专利号:US-7507861-B2 优先权日:2004-06-28 标题:Process for the preparation of atomoxetine hydrochloride 发明人:CASTELLI EUGENIO; LO MONACO GIUSEPPE; MANTOVANI SILVIA; DAVERIO PAOLA; RIVA PAOLO; VAILATI ALESSANDRA; BIANCHI STEFANO 权利人:TEVA PHARM FINE CHEMICALS SRL 摘要:The present invention provides improved processes for the preparation of atomoxetine hydrochloride under reaction conditions that improve reaction yields and facilitate commercial synthesis. In particular, the invention is directed to the synthesis of atomoxetine HCl by adding HCl to a mixture of (R)-(−)-tomoxetine (S)-(+)-mandelate with an organic solvent, with or without a base and water.
专利号:US-7439399-B2 优先权日:2004-06-28 标题:Processes for the preparation of atomoxetine hydrochloride 发明人:ARONHIME JUDITH; BIANCHI STEFANO; CASTELLI EUGENIO; DAVERIO PAOLA; MANTOVANI SILVIA; KOVACSNE-MEZEI ADRIENNE 权利人:TEVA PHARM FINE CHEMICALS SRL 摘要:The present invention provides improved processes for the preparation of atomoxetine hydrochloride under reaction conditions that improve reaction yields and facilitate commercial synthesis. In particular, the invention is directed to the synthesis of atomoxetine HCl by adding HCl to a mixture of (R)-(−)-tomoxetine (S)-(+)-mandelate with an organic solvent, with or without a base and water. In preferred embodiments, the atomoxetine hydrochloride produced is Form A.
专利号:US-4460501-A 优先权日:1983-08-30 标题 :Process for the synthesis of peptides utilizing thioxanthylmethyloxycarbonyl dioxides 发明人:CARPINO LOUIS A; SEGEV DAVID 权利人:RESEARCH CORP 摘要:A composition of the formula: ##STR1## wherein X is lower alkyl, and Z is an amino acid a peptide residue or a good leaving group, the composition is adaptable as a blocking or protecting group for an amine composition useful in peptide synthesis and a method of protecting an amino group of an organic molecule during a reaction which modifies a portion of the molecule other than the protected amino group.