CAS: 625-50-3; N-Ethylacetamide

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CAS号121-44-8 三乙胺 | CAS号60-35-5 乙酰胺 | CAS号74-96-4 溴乙烷 | CAS号75-04-7 乙胺 | CAS号64-19-7 冰醋酸 | CAS号96-29-7 2-丁酮肟 | CAS号141-78-6 乙酸乙酯 | CAS号84958-03-2 anti-Ethyl-meth... | CAS号78-93-3 甲乙酮 | CAS号625-77-4 二乙酰基胺 | CAS号1563-83-3 N-acetyl-N-ethy... | CAS号141-78-6 乙酸乙酯 | CAS号64-17-5 乙醇 | CAS号75-04-7 乙胺 | CAS号64-19-7 冰醋酸 | CAS号109-89-7 二乙胺 | CAS号81256-39-5 N-ethyl-3-pheny... | CAS号529-65-7 N-乙基乙酰苯胺 | CAS号55204-51-8 N-(1-methoxyeth...

N,N-二乙基乙酰胺置于硫酸,Iron(II) Sulfate,Hydroxylamine-O-Sulfonic Acid体系中,用 水 作为反应溶剂,化学反应 2.0H,反应生成 N-乙基乙酰胺
参考文献:Polar Effects In Free-Radical Reactions. Carbamoylation And .Alpha.-N-Amidoalkylation Of Heteroaromatic Bases By Amides And Hydroxylamine-O-Sulfonic Acid
标题:Polar Effects In Free-Radical Reactions. Carbamoylation And .Alpha.-N-Amidoalkylation Of Heteroaromatic Bases By Amides And Hydroxylamine-O-Sulfonic Acid
摘要:
DOI:10.1021/jo00192A022

专利信息

专利号:US-7589170-B1
优先权日:1998-09-25
标题 :Synthesis of cyclic peptides
发明人：SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER
权利人:UNIV QUEENSLAND
摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.

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:WO-9837078-A1
优先权日:1997-02-20
标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-7692019-B2
优先权日:2000-12-04
标 题:Methods for the stereoselective synthesis of substituted piperidines
发明人：AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HEFFERNAN MICHELE L R; HOEMANN MICHAEL Z; KESSLER DONALD W; SHAO LIMING; WU XINHE; XIE ROGER L
权利人:SEPRACOR INC
摘要:One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.

专利号:WO-0140193-A1
优先权日:1999-12-03
标题:Method for the synthesis of pyrazolines
发明人：BOLDI ARMEN M
权利人:CHEMRX ADVANCED TECHNOLOGIES I; BOLDI ARMEN M
摘要:The present invention provides a method for the synthesis of compounds of Formula (I). Also claimed are novel intermediates and their methods of synthesis.

专利号:US-2002103381-A1
优先权日:2000-11-30
标 题 :Method for the synthesis of pyrazolines
发明人：BOLDI ARMEN M
摘要:The present invention provides a method for the synthesis of compounds of Formula I: n n n Also claimed are novel intermediates and their methods of synthesis.