CAS: 700-49-2; 2-Fluoro-7H-Purin-6-Amine

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CAS号37076-78-1 2-氟-5-脱氧腺苷酸 | CAS号143482-58-0 6-azido-2-fluor... | CAS号109-80-8 1,3-丙二硫醇 | CAS号1904-98-9 2,6-二氨基嘌呤 | CAS号146-78-1 2-氟腺苷 | CAS号21679-12-9 2′-氟脱氧腺苷 | CAS号134217-15-5 9H-Purin-6-amin... | CAS号146-78-1 2-氟腺苷 | CAS号21679-12-9 2′-氟脱氧腺苷 | CAS号86626-06-4 3-(6-amino-2-fl...

2-氟-6-氯嘌呤置于乌洛托品,氨体系中,用 四氢呋喃,甲醇 作为反应溶剂,化学反应 46.0H,以65%的收率获得产物2-氟-6-氨基嘌呤
参考文献:开发一条商业化生产路线,以2-氟丁烯酸为基础,这是islatravir的关键非天然核碱基
标题:开发一条商业化生产路线,以2-氟丁烯酸为基础,这是islatravir的关键非天然核碱基
摘要:我们报告了islatravir(mk-8591),一种新型的核苷逆转录酶易位抑制剂(nrtti)的关键片段的实际合成,该抑制剂目前正在研究中,针对hiv感染的治疗和暴露前预防(prep).该片段(非天然核碱基2-氟腺嘌呤)通过生物催化的羟醛糖基化级联反应并入mk-8591,这对其合成和分离提出了严格的要求.本文介绍的是开发从鸟嘌呤到实用,可扩展路线的开发工作,其特征在于采用双氟化方法开发新颖的9-Thp-2,6-二氟嘌呤中间体,从而实现温和,高度选择性的直接胺化.这种一锅式氟化/胺化步骤利用直接分离来提供高纯度的9-Thp-2-氟腺嘌呤,在反应性,溶解性和结晶度方面具有理想的特性.在水性缓冲液中酸催化的2-氟腺嘌呤释放可提供适当的纯度,以利于酶联级联反应进入mk-8591.
DOI:10.1021/acs.Oprd.0C00304

专利信息

专利号:US-2024287520-A1
优先权日:2021-06-30
标题:Method for synthesis of linkage modified oligomeric compounds
发明人：RODRIGUEZ ANDREW A
权利人:IONIS PHARMACEUTICALS INC
摘要:The present disclosure provides methods of synthesizing modified oligonucletodies and oligomeric compounds (including oligomeric compounds that are antisense agents or portions thereof) comprising a modified oligonucleotide having at least one modified internucleoside linking group. In certain embodiments, the present disclosure provides stabilized formulations of certain sulfonyl azides for use in the synthesis of olignonucleotides comprising one or more sulfonyl phosphoramidate linkages. Some embodiments provide stabilized compositions of high energy reagents that may be used in the synthesis of modified oligonucleotides, allowing for safe process scale preparation thereof.

专利号:US-2004242897-A1
优先权日:2002-07-31
标题 :Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-10751419-B2
优先权日:2014-05-01
标题:Method for synthesis of reactive conjugate clusters
发明人：MIGAWA MICHAEL T; YU JINGHUA; WAN W BRAD; PATEL SAYTEN P; VASQUEZ GUILLERMO; KINBERGER GARTH A; PRAKASH THAZHA P; SETH PUNIT P; SWAYZE ERIC E
权利人:IONIS PHARMACEUTICALS INC
摘要:Provided herein are improved methods for the synthesis of reactive conjugate clusters and intermediates used in such methods. In particular, improvements are provided that enhance the synthesis of reactive conjugate clusters by reducing the number of synthetic steps required. The reactive conjugate clusters prepared using the improved methods don't include any transacylation impurities that are formed using existing methods. The improved methods also provide an increase in overall yield and a cost benefit over existing methods.

专利号:WO-2004011474-A1
优先权日:2002-07-31
标题:Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-6653468-B1
优先权日:2002-07-31
标 题 :Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH
权利人:ISIS PHARMACEUTICALS INC
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-12037623-B2
优先权日:2018-07-09
标 题 :Enzymatic synthesis of 4′-ethynyl nucleoside analogs
发明人：HUFFMAN MARK A; FRYSZKOWSKA ANNA; KOLEV JOSHUA N; DEVINE PAUL N; CAMPOS KEVIN R; TRUPPO MATTHEW; NAWRAT CHRISTOPHER C
权利人:MERCK SHARP & DOHME; MERCK SHARP & DOHME LLC
摘要:The present invention relates to an enzymatic synthesis of 4′-ethynyl-2′-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make said compounds. It also relates to the novel intermediates employed in the process.