CAS: 34408-14-5; (2R,3R,4S,5R)-2-(6-Amino-8-Chloro-9H-Purin-9-yl)-5-(Hydroxymethyl)Tetrahydrofuran-3,4-Diol

相似化合物

146-77-0 146-78-1 21679-14-1

上下游产品

adenosine water 6-BenzyladenosineN6-Benzyladenosine 8-mercaptoadenosine 6-phenoxyacetyl-8-chloroadenosineN6-phenoxyacetyl-8-chloroadenosine N-(9-{5-[bis-(4-methoxy-phenyl)-phenyl-methoxymethyl]-3,4-dihydroxy-tetrahydro-furan-2-yl}-8-chloro-9H-purin-6-yl)-2-phenoxy-acetamideN-(9-{5-[bis-(4-methoxy-phenyl)-phenyl-methoxymethyl]-3,4-dihydroxy-tetrahydro-furan-2-yl}-8-chloro-9H-purin-6-yl)-2-phenoxy-acetamide N-{9-[5-[bis-(4-methoxy-phenyl)-phenyl-methoxymethyl]-4-(tert-butyl-dimethyl-silanyloxy)-3-hydroxy-tetrahydro-furan-2-yl]-8-chloro-9H-purin-6-yl}-2-phenoxy-acetamideN-{9-[5-[bis-(4-methoxy-phenyl)-phenyl-methoxymethyl]-4-(tert-butyl-dimethyl-silanyloxy)-3-hydroxy-tetrahydro-furan-2-yl]-8-chloro-9H-purin-6-yl}-2-phenoxy-acetamide N-{9-[5-[bis-(4-methoxy-phenyl)-phenyl-methoxymethyl]-3-(tert-butyl-dimethyl-silanyloxy)-4-hydroxy-tetrahydro-furan-2-yl]-8-chloro-9H-purin-6-yl}-2-phenoxy-acetamideN-{9-[5-[bis-(4-methoxy-phenyl)-phenyl-methoxymethyl]-3-(tert-butyl-dimethyl-silanyloxy)-4-hydroxy-tetrahydro-furan-2-yl]-8-chloro-9H-purin-6-yl}-2-phenoxy-acetamide

📜8-Mercaptoadenosine置于n-氯代丁二酰亚胺体系中,用 甲醇 作为反应溶剂,化学反应 3.0H,以52%的收率获得产物8-氯腺嘌呤核苷
参考文献:α,β-Methylene-Adp (Aopcp) Derivatives And Analogues: Development Of Potent And Selective Ecto-5'-Nucleotidase (Cd73) Inhibitors
标题:α,β-Methylene-Adp (Aopcp) Derivatives And Analogues: Development Of Potent And Selective Ecto-5'-Nucleotidase (Cd73) Inhibitors
摘要:Ecto-5'-Nucleotidase (En,Cd73) Catalyzes The Hydrolysis Of Extracellular Amp To Adenosine. En Inhibitors Have Potential For Use As Cancer Therapeutics. The En Inhibitor Alpha,Beta-Methylene-Adp (Aopcp,Adenosine-5'-O-[(Phosphonomethyl)Phosphonic Acid]) Was Used As A Lead Structure,And Derivatives Modified In Various Positions Were Prepared. Products Were Tested At Rat Recombinant En. 6-(Ar)Alkylamino Substitution Led To The Largest Improvement In Potency. N-6-Monosubstitution Was Superior To Symmetrical N-6,N-6-Disubstitution. The Most Potent Inhibitors Were N-6-(4Chlorobenzyl)-(10L,Psb-12441,K-I 7.23 N.M),N-6-Phenylethyl(10H,Psb-12425,K-I 8.04 Nm),And N-6-Benzyl-Adenosine-5'-O[(Phosphonomethyl)Phosphonic Acid] (10G,Psb-12379,K-I 9.03 Nm). Replacement Of The 6-Nh Group In 10G By 0 (10Q,Psb-12431) Or S (10R,Psb-12553) Yielded Equally Potent Inhibitors (10Q,9.20 Nm; 10R,9.50 Am). Selected Compounds Investigated At The Human Enzyme Did Not Show Species Differences; They Displayed High Selectivity Versus Other Ecto-Nudeotidases And Adp-Activated P2Y Receptors. Moreover,High Metabolic Stability Was Observed. These Compounds Represent The Most Potent En Inhibitors Described To Date.
DOI:10.1021/acs.Jmedchem.5B00802

专利信息

专利号:WO-2020128469-A1
优先权日:2018-12-19
标 题 :Synthesis of 8-chloroadenosine derivatives including nuc-9701
发明人：GARLAPATI RAMESH; KOTALA MANI BUSHAN; EVANS JAMES; KENNOVIN GORDON
权利人:NuCana plc
摘要:The present invention generally relates to a novel process for the preparation of 8-chloroadenosine derivatives, and particularly NUC-9701(8-chloroadenosine-5'-O- [naphthyl(benzyloxy-L-alaninyl)] phosphate) an anticancer ProTide of 8-chloroadenosine.

专利号:US-12054511-B2
优先权日:2017-06-14
标题 :Synthesis of phosphate derivatives
发明人：GRIFFITH HUGH; KENNOVIN GORDON; DAMMALAPATI VENKATA LAKSHMI NARASIMHA RAO; KOTALA MANI BUSHAN
权利人:NuCana plc
摘要:The present invention is a process for the preparation of certain 5′-phosphoramidate nucleotide diastereoisomers. The phosphoramidates include those useful in the treatment of cancer such as NUC-3373 (5-fluoro-2′-deoxyuridine-5′-O-[1-naphthyl(benzyloxy-L-alaninyl)]phosphate].

专利号:US-2022402962-A1
优先权日:2017-06-14
标题 :Synthesis of phosphate derivatives

专利号:US-2020181186-A1
优先权日:2017-06-14
标 题:Synthesis of phosphate derivatives

专利号:US-2020123190-A1
优先权日:2017-04-25
标题 :5'-position dibenzyl monophosphate derivative of nucleoside-based anticancer agent or antivirus agent
发明人：SAKO MAGOICHI
权利人:OHARA PHARMACEUTICAL CO LTD
摘要:To provide, in place of injected agents (nucleoside-based anticancer agents or antivirus agents) clinically used as therapeutic drugs for cancer or virus infections, a medicine that has high stability with respect to various hydrolytic metabolic enzymes, is absorbed into the body even by oral administration, and exhibits a cytocidal effect by being incorporated into a DNA and RNA biosynthetic route and inhibiting the modification and extension of DNA and RNA or inhibiting reverse transcriptases or inhibiting protein synthesis. n The aforementioned problem is solved by a novel compound represented by formula (I). (In the formula, D is the 5′-position moiety of a nucleoside-based anticancer agent or an antivirus agent, and R 1 and R 2 are each a benzyl group that may have the same substituent or different substituents.)

专利号:US-11759496-B2
优先权日:2016-05-10
标题:Compounds and pharmaceutical use thereof in the treatment of cancer
发明人：SUSIN SANTOS A; KAROYAN PHILIPPE; MERLE-BERAL HÉLÈNE
权利人:KAROYAN PHILIPPE
摘要:The present invention relates to a compound or a pharmaceutical salt thereof comprising a hexapeptide sequence of formula (I), its method of synthesis and its use in anticancer therapy. The invention also relates to a pharmaceutical composition for use in the treatment of cancer comprising at least one soluble peptide according to the invention or at least one acid nucleic according to the invention or at least one expression vector according to the invention, or at least one host cell according to the invention and a pharmaceutically acceptable carrier.