CAS: 39929-79-8; 7H-Pyrrolo[2,3-D]Pyrimidine-2,4-Diol

上下游产品

4-Amino-2,6-dihydroxy-5-(2,2-diethoxy-ethyl)-pyrimidin 2-chloroethanal 4-Amino-2,6-dihydroxypyrimidine 6-amino-2,4-dihydroxypyrimidine 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine 2-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-ol 2-((2-chloro-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-3-yl)methyl)benzonitrile 2-((2-chloro-7-methyl-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-3-yl)methyl)benzonitrile

2,4-二甲氧基-7H-吡咯并[2,3-D]嘧啶置于盐酸体系中,用 1,4-二氧六环 用作溶剂,化学反应生成2,4-二羟基吡咯[2,3-D]嘧啶
参考文献:Ara-7-Deazaxanthosine-具有稳定n-糖基键的黄嘌呤核苷
标题:Ara-7-Deazaxanthosine-具有稳定n-糖基键的黄嘌呤核苷
摘要:Ara-7-Deazaxanthosine(2)的制备是通过相转移糖基化的2,4-二甲氧基-7 ħ吡咯并[2,3-D ]嘧啶(图5B与halogenose)6.用三氯化硼除去优选在糖基化反应中形成的β-端基异构体8的苄基保护基,并用酸分离出2,4-二甲氧基.与黄嘌呤(1A)相反,7-脱氮嘌呤核苷2具有在酸水解时稳定的n-糖基键.通过比较嘌呤核苷与2的动力学参数描述了质子催化水解的反应机理,也解释了吡咯并[2,3-D ]嘧啶核苷2的稳定性.
Doi:10.1002/jlac.198419840210

专利信息

专利号:US-6639059-B1
优先权日:1999-03-24
标 题 :Synthesis of [2.2.1]bicyclo nucleosides
发明人：KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M
权利人:EXIQON AS
摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs.

专利号:US-6734291-B2
优先权日:1999-03-24
标题:Synthesis of [2.2.1]bicyclo nucleosides
发明人：KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M
权利人:EXIQON AS
摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs

专利号:EP-1501848-B1
优先权日:2002-05-08
标 题 :Synthesis of locked nucleic acid derivatives
发明人：SORENSEN MADS DETLEF; WENGEL JESPER; KOCH TROELS; CHRISTENSEN SIGNE M; ROSENBOHM CHRISTOPH; PEDERSEN DANIEL SEJER
权利人:SANTARIS PHARMA AS
摘要:The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as alpha-L-oxy-LNA, amino-LNA, alpha-L-amino-LNA, thio-LNA, alpha-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues. (Formula I)

专利号:US-7915201-B2
优先权日:2003-03-20
标 题:Ligational encoding of small molecules
发明人：FRANCH THOMAS; JACOBSEN SOEREN NYBOE; RASMUSSEN TORBEN RAVN; NEVE SOEREN; PEDERSEN HENRIK; GOULIAEV ALEX HAAHR
权利人:NUEVOLUTION AS
摘要:The invention relates to a method for synthesising a bifunctional complex comprising an encoded molecule and an identifier polynucleotide identifying the chemical entities having participated in the synthesis of the encoded molecule, said method comprising the steps of i) providing a) at least one template comprising one or more codons capable of hybridising to an anti-codon, wherein said template is optionally associated with one or more chemical entities, and b) a plurality of building blocks each comprising an anti-codon associated with one or more chemical entities, and ii) hybridising the anti-codon of one or more of the provided building blocks to the template, iii) covalently linking said anti-codons and/or linking the at least one template with the anti-codon of at least one building block, thereby generating an identifier polynucleotide capable of identifying chemical entities having participated in the synthesis of the encoded molecule, iv) separating the template from one or more of the anti-codons hybridised thereto, thereby generating an at least partly single stranded identifier polynucleotide associated with a plurality of chemical entities, v) generating a bifunctional complex comprising an encoded molecule and an identifier polynucleotide identifying the chemical entities having participated in the synthesis of the encoded molecule, wherein said encoded molecule is generated by reacting at least two of said plurality of chemical entities associated with the identifier polynucleotide, and wherein said at least two chemical entities are provided by separate building blocks.

专利号:US-8309716-B2
优先权日:2005-07-29
标题 :Pyrrolo[2,3-d]pyrimidine derivatives: their intermediates and synthesis
发明人：RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J
权利人:RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J; PFIZER
摘要:This invention relates to methods and intermediates useful for the synthesis of pyrrolo[2,3-d]pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.

专利号:US-10730906-B2
优先权日:2002-08-01
标题:Multi-step synthesis of templated molecules
发明人：PEDERSEN HENRIK
权利人:PEDERSEN HENRIK; NUEVOLUTIONS AS
摘要:Disclosed is a method for the manufacture of a library of complexes. The complexes comprise templated molecules attached to the template which directed the synthesis thereof. The templated molecules are produced in a step-by-step fashion which provides for a high local concentration of reactive groups involved in the formation of connections between the individual components of the template molecule.