CAS: 658-78-6; 4-Nitrophenyl 2,2,2-Trifluoroacetate

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CAS号100-02-7 对硝基苯酚 | CAS号108-24-7 乙酸酐 | CAS号407-25-0 三氟乙酸酐(TFAH) | CAS号51599-76-9 N-trifluoroacet... | CAS号183266-61-7 (三氟乙酰基)苯并三唑 | CAS号108818-44-6 (4-nitrophenyl)... | CAS号33755-53-2 (+)-生物素4-硝基苯酯 | CAS号100-02-7 对硝基苯酚 | CAS号76-05-1 三氟乙酸(TFA) | CAS号7763-16-8 Z-谷氨酰胺对硝基苯酯 | CAS号73785-43-0 6-羧基己基磷酸胆碱对硝基苯酯 | CAS号15387-45-8 2-叔丁氧羰基氨基-4-氨基甲... | CAS号13574-81-7 Z-GLY-GLY-ONP | CAS号2483-49-0 N-叔丁氧羰基-L-丙氨酸 4-硝基苯酯 | CAS号1492-30-4 棕榈酸对硝基苯酯

📜4-硝基碘苯置于1,10-菲罗啉,Silver Trifluoromethanesulfonate,间氯过氧苯甲酸体系中,用 1,2-二氯乙烷,乙腈 作为反应溶剂,化学反应 20.58H,反应生成 对硝基三氟乙酸苯酯
参考文献:银催化非反应性羧酸酯的偶联:α-氟化 O-芳基酯的合成
标题:银催化非反应性羧酸酯的偶联:α-氟化 O-芳基酯的合成
摘要:由于其低反应活性,α-氟化芳基酯在通过 α-氟化羧酸酯的o-芳基化合成中提出了挑战.通过将银催化剂与芳基(三甲氧基苯基)碘鎓甲苯磺酸盐组合以得到α-氟化芳基酯,解决了这一限制.我们设想催化系统涉及通过银(i)盐氧化产生的高价芳基银物质.本方法提供了各种α-氟化芳基酯(包括药物衍生物的氟化类似物)的合成方案.
DOI:10.1021/acs.Orglett.4C01731

专利信息

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-9193691-B2
优先权日:2012-04-27
标题:Methods for the synthesis of activated ethylfumarates and their use as intermediates
发明人：KRAFT KELLY SULLIVAN; FREEMAN JOHN J; SERWINSKI PAUL; PAVIA VINNIE; PHANSTIEL OTTO; KAUR NAVNEET
权利人:MANNKIND CORP; MANNKIND CORP
摘要:Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphosphoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput.

专利号:US-4849513-A
优先权日:1983-12-20
标 题 :Deoxyribonucleoside phosphoramidites in which an aliphatic amino group is attached to the sugar ring and their use for the preparation of oligonucleotides containing aliphatic amino groups
发明人：SMITH LLOYD M; FUNG STEVEN; KAISER ROBERT J
权利人:CALIFORNIA INST OF TECHN
摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.

专利号:US-5118802-A
优先权日:1983-12-20
标 题:DNA-reporter conjugates linked via the 2' or 5'-primary amino group of the 5'-terminal nucleoside
发明人：SMITH LLOYD M; FUNG STEVEN; KAISER JR ROBERT J
权利人:CALIFORNIA INST OF TECHN
摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.

专利号:US-5712269-A
优先权日:1993-04-05
标题 :M2 receptor ligand for the treatment of neurological disorders
发明人：MCCABE R TYLER; WILSON BRYAN R; RHODES CHRISTOPHER A
权利人:PHARMACEUTICAL DISCOVERY CORP
摘要:Muscarinic M2 receptor ligands are described which are suitable for the treatment of neurological disorders, and which may be administered with minimal side-effects. A method of synthesis of these compounds is also described.

专利号:US-7408075-B1
优先权日:2005-03-23
标 题:Synthesis of phosphocholine ester derivatives and conjugates thereof
发明人：REZANKA LOUIS J
权利人:US HEALTH
摘要:Aspects of the present invention include methods of synthesizing phosphocholine analogues and the phosphocholine conjugates formed therefrom and their use in preventing infections caused by microorganisms.