CAS: 1651-29-2; 6-Chloro-2-Fluoro-9H-Purine

相似化合物

87-42-3 5451-40-1 18552-90-4

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2-氨基-6-氯嘌呤 2-Amino-6-Chloropurin 10310-21-1

2-氨基-6-氯嘌呤置于氢氟酸,亚硝酸特丁酯体系中,用 吡啶 用作溶剂,化学反应 0.33H,以42%的收率获得2-氟-6-氯嘌呤
参考文献:新型非核苷酸嘌呤衍生物作为 P2X7 拮抗剂治疗神经炎症的合成及药理评价
标题:新型非核苷酸嘌呤衍生物作为 P2X7 拮抗剂治疗神经炎症的合成及药理评价
摘要:Atp 门控 P2X7 嘌呤能受体 (P2X7) 参与许多神经退行性疾病 (Ndd) 的发病机制.已经开发了几种 P2X7 拮抗剂,但没有一种达到该适应症的临床试验.在这项工作中,我们设计并合成了新型血脑屏障(bbb)渗透性衍生物作为潜在的 P2X7 拮抗剂.它们包含通过不同的短间隔基与芳基连接的嘌呤或黄嘌呤核心.在表达人 P2X7 的 Hek293 细胞系中的 Yo-Pro-1 摄取测定和细胞内钙动力学,非洲爪蟾卵母细胞中的两电极电压钳记录以及小鼠腹膜巨噬细胞中的白细胞介素 1β 释放测定中测试了化合物.通过平行人工膜渗透性测定和 P-糖蛋白 Atp 酶活性评估 Bbb 渗透性.二氯芳基嘌呤基乙醇具有一定的 P2X7 阻断作用,为化合物6 (2-(6-氯-9 H-嘌呤-9-基)-1-(2,4-二氯苯基)乙烷-1-酮),命名为 Ith15004,是最有效的,选择性且 Bbb 通透性拮抗剂.
Doi:10.1021/acs.Jmedchem.0C02145

专利信息

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-2006009642-A1
优先权日:2001-10-12
标题 :Methods for the synthesis of substituted purines
发明人：DING SHENG; DING QIANG; GRAY NATHANAEL S; SCHULTZ PETER G
权利人:IRM LLC
摘要:The invention provides general methods for preparing 2,9-, 2,6,9-, O 6 -aryl- and O 6 -alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments, Mitsunobu alkylation of 2-fluoro-6-phenylsulfenylpurine at N9 with alcohols in solution, followed by C2-capture of the purine core with a resin-bound amine and subsequent oxidation and displacement of the C6 sulfonyl group with amines and anilines.

专利号:US-5118800-A
优先权日:1983-12-20
标 题 :Oligonucleotides possessing a primary amino group in the terminal nucleotide
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-2023104823-A1
优先权日:2020-01-22
标 题:Process for the preparation of purine derivatives exhibiting cdk inhibitory activity
发明人：SKEAD BENJAMIN; LONDESBROUGH DEREK; GILL CHRIS; HUDSON ALEX
权利人:CYCLACEL LTD
摘要:The present invention relates to a process for preparing a compound of formula [I], or a pharmaceutically acceptable salt thereof, said process comprising the steps of: (i) forming a reaction mixture comprising a compound of formula [II] and a compound of formula [III]; (ii) heating said reaction mixture to a temperature of at least about 130° C. to form a compound of formula [I]; (iii) isolating said compound of formula [I] from the mixture and optionally recovering unreacted compound of formula [III]; and (iv) optionally converting said compound of formula [I] into salt form; wherein: R1 and R2 are each independently H, alkyl or haloalkyl; R3 and R4 are each independently H, alkyl, haloalkyl or aryl; R5 is alkyl, alkenyl, cycloalkyl or cycloalkyl-alkyl, each of which may be optionally substituted with one or more OH groups; R6 is selected from cyclopropylamino, cyclopropylmethylamino, cyclobutylamino, cyclobutylmethylamino and where one of X, Y and Z is N and the remainder are CR9; R7, R8 and each R9 are independently H, alkyl or haloalkyl, wherein at least one of R7, R8 and R9 is other than H. Further aspects of the invention relate to a process for preparing intermediates of formula [II], and other intermediates useful in the synthesis of compounds of formula [I].

专利号:US-6949644-B2
优先权日:2001-10-12
标题 :Methods for the synthesis of substituted purines
发明人：DING SHENG; DING QIANG; GRAY NATHANAEL S; SCHULTZ PETER G
权利人:SCRIPPS RESEARCH INST
摘要:The invention provides general methods for preparing 2,9-, 2,6,9-, O 6 -aryl- and O 6 -alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments, Mitsunobu alkylation of 2-fluoro-6-phenylsulfenylpurine at N9 with alcohols in solution, followed by C2-capture of the purine core with a resin-bound amine and subsequent oxidation and displacement of the C6 sulfonyl group with amines and anilines. In one aspect, the present invention provides a method of preparing a 2,6,9-substituded purine compounds of Formula I: n n nthe method comprising:n a) oxidizing a resin-bound compound of Formula II: n n to provide a resin-bound compound of Formula III: n n b) reacting the compound of Formula III with an amine of Formula IVn nNR 3 R 4   IV,n nto provide a resin-bound compound of Formula V n n c) cleaving the resin-bound compound of Formula V from the resin to provide the substituted purine compounds of Formula I.