CAS: 19690-23-4; 6-Iodo-9H-Purin-2-Amine

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CAS号10310-21-1 2-氨基-6-氯嘌呤 | CAS号7440-44-0 活性炭 | CAS号132194-23-1 (2S)-5α-(2-Amin...

2-氨基-6-氯嘌呤置于氢碘酸体系中,用 水 用作溶剂,以77 %的收率获得2-氨基-6-碘嘌呤
参考文献:Fraglites-最小的,卤代的碎片,显示药效基团双峰.一种有效的药物可及性评估和命中方法.
标题:Fraglites-最小的,卤代的碎片,显示药效基团双峰.一种有效的药物可及性评估和命中方法.
摘要:鉴定蛋白质上的配体结合位点是基于靶标的药物发现中的关键步骤.当前的解决方法要求对铅样或片段分子的大型文库进行资源密集型筛选.在这里,我们描述了一种高效而有效的实验方法,用于使用一组表达成对的氢键基序的卤化化合物(称为fraglite)来绘制相互作用位点.Fraglite利用卤素取代基的反常散射,识别出类似于药物的生产性相互作用,通过x射线晶体学可以灵敏而明确地识别出这种相互作用.蛋白质相互作用表面的这种作图提供了可药用性的评估,并且可以为结合相互作用基序的命中分子的从头设计确定有效的起点.通过对细胞周期蛋白依赖性激酶2作图来说明该方法,该激酶成功鉴定了正构和变构位点.命中被迅速完善,以开发有效的铅样分子.因此,该方法提供了一种识别配体位点,评估易加工性和发现新线索的新方法.
Doi:10.1021/acs.Jmedchem.9B00304

专利信息

专利号:US-7189849-B2
优先权日:1997-02-10
标 题:Synthesis of acyclic nucleoside derivatives
发明人：LEANNA M ROBERT; RASMUSSEN MICHAEL; HANNICK STEVEN M; TIEN JIEN-HEH J; LUKIN KIRILL A; TIAN ZHENPING; CHANG SOU-JEN; CURTY CYNTHIA B; NARAYANAN BIKSHANDARKOIL A; BELLETTINI JOHN; SHELAT BHADRA; SPITZ TIFFANY
权利人:MEDIVIR AB
摘要:Novel processes towards the synthesis of the antiviral valomaciclovir stearate in which an esterified guanine acetal is reduced to the corresponding alcohol, reacted with an activated amino acid and N-deprotected. The esterified guanine acetal is prepared from a 9-guanine derivative bearing an acyclic hydroxymethylbutylacetal. The processes are amendable to one-pot reactions.

专利号:US-6316228-B1
优先权日:1996-10-21
标题 :Efficient synthesis of nucleosides
发明人：NAIR VASU; PAL SURESH
权利人:UNIV IOWA RES FOUND
摘要:Methods and compositions, including cell cultures, for producing nucleosides are provided which comprise contacting a nucleoside precursor and a sugar moiety donor with a cell containing a nucleoside phosphorylase. The nucleoside precursor can be a purine or pyrimidine base and the sugar moiety donor can comprise a ribose, a deoxyribose, including 2-deoxyribose, or other sugar of choice. The methods and composition can be used to make thymidine from thymine and 2-deoxyinosine or 2′-deoxyadenosine. Other nucleosides, including those having anticancer and/or antiviral properties, also can be obtained according to the invention.

专利号:US-5440037-A
优先权日:1991-11-22
标题 :Method for production of 2-amino-6-halogenopurine derivatives
发明人：IGI MASAMI; HAYASHI TAKETO
权利人:SUMIKA FINE CHEMICALS CO LTD
摘要:The present invention is directed to a method for production of a 2-amino-6-halogenopurine, a novel synthesis intermediate therefor and a method for production of said synthesis intermediate. The desired 2-amino-6-halogenopurine is an intermediate for the production of the compounds useful as antiviral agents, and by using the compound of the present invention as a starting material, the 2-amino-6-halogenopurine can be produced in high yield.

专利号:US-7411065-B2
优先权日:2002-04-26
标 题 :PNA monomer and precursor
发明人：KIM SUNG KEE; LEE HYUNIL; LIM JONG CHAN; CHOI HOON; JEON JAE HOON; AHN SANG YOUL; LEE SUNG HEE; YOON WON JUN
权利人:PANAGENE INC
摘要:This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oglimers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: n nwhereinn E is nitrogen or C—R′; J is sulfur or oxygen; R′, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural α-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.

专利号:US-2004024214-A1
优先权日:1997-02-10
标 题 :Synthesis of acyclic nucleoside derivatives

专利号:US-2004248910-A1
优先权日:1997-02-10
标题:Synthesis of acyclic nucleoside derivatives