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Highly efficient chemical phosphorylation of 6-(4-phenylpiperazine-1-yl)-9-(β-D-ribofuranosyl)-9H-purine
Nucleosides, Nucleotides & Nucleic Acids ( IF 1.1 ) Pub Date : 2021-01-08 , DOI: 10.1080/15257770.2020.1843679
M. Fatih Polat 1 , Meral Tuncbilek 2
Affiliation  

Antimetabolites, which are metabolic antagonists used in the treatment of cancer and viral diseases by replacing metabolites, inhibit the action of metabolic enzymes and disrupt the pathways of synthesis of structural units necessary for the formation of nucleic acids. Purine antagonists, that are subunits of antimetabolites, reduce the production of purine bases, and hence, cause the nucleotide production to stop and bring about the death of cancer cells. Fludarabine (2-fluoro-ara-AMP), which is used in chemotherapy, is an antimetabolite of the purine class containing mono phosphate in its structure. In this study, a protocol was presented to effectively and efficiently synthesis of 6-(4-phenylpiperazine-1-yl)-9-(β-D-ribofuranosyl)-9H-purine-5'- O-phosphate compound in six steps and 25% overall yield starting with commercially available 6-chloropurine.

中文翻译:

6-(4-苯基哌嗪-1-基)-9-(β-D-呋喃核糖基)-9H-嘌呤的高效化学磷酸化

抗代谢物是一种代谢拮抗剂,用于通过替代代谢物来治疗癌症和病毒性疾病,抑制代谢酶的作用并破坏形成核酸所必需的结构单元的合成途径。嘌呤拮抗剂是抗代谢物的亚单位,可减少嘌呤碱基的产生,从而导致核苷酸产生停止并导致癌细胞死亡。用于化疗的氟达拉滨 (2-fluoro-ara-AMP) 是一种嘌呤类的抗代谢物,其结构中含有单磷酸酯。在这项研究中,提出了一个协议,以有效和高效地合成 6-(4-phenylpiperazine-1-yl)-9-(β-D-ribofuranosyl)-9H-purine-5'
更新日期:2021-01-08
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