CAS: 6736-58-9; 3-Deazaadenosine

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86583-19-9 58-61-7 5536-17-4

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3,4-二氨基吡啶置于hydrazine Hydrate,氨,四氯化锡,间氯过氧苯甲酸,三氯氧磷体系中,用 甲醇,二氯甲烷,乙腈 作为反应溶剂,化学反应 34.5H,反应生成 3-脱氮腺苷
参考文献:全家族分析的氨酰基-氨磺酰基-3-Deazaadenosine类似物作为氨酰基-Trna合成酶的抑制剂
标题:全家族分析的氨酰基-氨磺酰基-3-Deazaadenosine类似物作为氨酰基-Trna合成酶的抑制剂
摘要:氨酰基-Trna合成酶(aarss)是一种将氨基酸精确地与其同源trna相连的酶.如果可以鉴定出物种选择性抑制剂,则该过程对于蛋白质翻译至关重要,被认为是开发新型抗菌剂的可行目标.氨酰基氨磺酰酰基腺苷(aasas)是强直向同源物特异性aars抑制剂,在体外表现出纳摩尔亲和力,但吸收受限.继我们之前关于碱基部分取代的工作之后,我们评估了n 3的作用通过合成相应的3-脱氮杂腺苷类似物(aas3Das)将腺嘌呤定位在-位.一个典型的生物具有20种不同的aars,可以将其分为两个不同的结构类别.因此,我们通过氨基磺酸桥将六种不同的氨基酸(均等地靶向两种酶)偶联到3-Deazaadenosine.在评估所获得的类似物的抑制能力时,注意到明显的类别偏倚,与等效的aasa相比,针对ii类酶的aas3Da类似物的活性丧失.对可用晶体学结构的评估指出了保守水分子的存在,该分子对于ii类酶中的碱基识别可能具有
DOI:10.1016/j.Ejmech.2018.02.013

专利信息

专利号:US-11858953-B2
优先权日:2018-04-04
标 题:Compositions and methods for synthesis of phosphorylated molecules
发明人：CHAPUT JOHN; LIAO JEN-YU; BALA SAIKAT
权利人:UNIV CALIFORNIA
摘要:The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.

专利号:US-7635772-B2
优先权日:2002-12-18
标 题 :Process for the preparation of oligonucleotides
发明人：MCCORMAC PAUL
权利人:AVECIA BIOTECHNOLOGY INC
摘要:A process for the synthesis of an oligonucleotide is provided in which an oligonucleotide is assembled on a swellable solid support using the phosphoramidite approach in the presence of an activator, wherein the activator is not tetrazole or a substituted tetrazole. Preferred activators are pyridinium, imidazolinium and benzimidazolinium salts; benzotriazole and derivatives thereof; and saccharin or a saccharin derivative. Preferred swellable solid supports comprise functionalised polystyrene, partially hydrolysed polyvinylacetate or poly(acrylamide).

专利号:US-4347315-A
优先权日:1980-04-25
标 题 :Synthesis of ribosides using bacterial phosphorylase
发明人：KRENITSKY THOMAS A; RIDEOUT JANET L
权利人:BURROUGHS WELLCOME CO
摘要:4-Substituted-3-deazapurine ribosides are prepared by the enzymatically catalyzed reaction of 4-substituted-3-deazapurine with a ribose donor.

专利号:EP-0038568-B1
优先权日:1980-04-23
标题 :Synthesis of deazapurine nucleosides
摘要:A method for the preparation of 4-substituted-1- beta -D-ribofuranosyl-1H-imidazo- [4,5-c)-pyridines by enzymatic ribosylation of the corresponding 4-substituted-1H-imidazo-[4,5-c]-pyridine is disclosed. In particular the preparation of 4-amino-1- beta -D-ribofuranosyl-1H-imidazo-[4,5-c]-pyridine (3-deazadenosine) is described.

专利号:JP-5714490-B2
优先权日:2008-09-06
标题:Methods for preparing oligonucleotides by RNA synthesis, phosphoramidites for synthetic RNA in the reverse direction, and bond formation in the 5 'to 3' direction for synthesis of RNA oligomers

专利号:US-7247720-B2
优先权日:2002-10-15
标题:Phosphitylation process
发明人：SINHA NANDA DULAL
权利人:AVECIA BIOTECHNOLOGY INC
摘要:A process for the phosphitylation of an alcohol or thiol with a phosphitylation agent in the presence of an activator is provided. The activator has the formula: n nwherein p is 0 or an integer from 1 to 4 and R for each occurrence is a substituent. Preferably X 7 is O and p is 0. The activator is commonly employed as a salt complex with an organic base. Preferred alcohols or thiols include nucleosides and oligonucleotides. The process is particularly suited for the synthesis of phosphoramidites.