63205-44-7Relevant academic research and scientific papers
NOVEL 6-SUBSTITUTED 7-DEAZAPURINES AND CORRESPONDING NUCLEOSIDES AS MEDICAMENTS
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Page/Page column 25-26; 28; 48, (2021/08/27)
The present invention relates to the synthesis of 6-substituted 7-deazapurines and their corresponding nucleosides by coupling aryl or alkyl Grignard reagents with halogenated purine nucleosides in the presence of iron or an iron/copper mixture such as Fe(acac)3/Cul. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of said pharmaceutical compositions to treat or prevent viral infections.
Method for catalytically synthesizing 7-denitrified purine compound by using iron coordination compound
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Paragraph 0063-0067, (2021/10/27)
The invention relates to a method for catalytically synthesizing a 7-denitrogenated purine compound by using an iron coordination compound. The method comprises the following steps: in the presence of an alkali, taking 7-denitrogenated purine and halogenated hydrocarbon as raw materials, taking an iron coordination compound containing an ortho-carborane benzoxazole structure as a catalyst, and reacting at room temperature to obtain the 6-substituted 7-denitrogenated purine compound. Compared with the prior art, the method has the advantages that the iron coordination compound containing the ortho-carborane benzoxazole structure is utilized to catalytically synthesize the 6-substituted 7-deazapurine compound, so that the compound is prepared by a one-pot method at room temperature, the use equivalent of the catalyst is low, the reaction condition is mild, the raw materials are cheap and easy to obtain, the substrate universality is high, and the yield is high.
Iron/Copper Co-Catalyzed Cross-Coupling Reaction for the Synthesis of 6-Substituted 7-Deazapurines and the Corresponding Nucleosides
Daelemans, Dirk,Herdewijn, Piet,Li, Qingfeng,Persoons, Leentje
, (2020/01/03)
An efficient access to 6-substituted 7-deazapurine and the corresponding nucleosides by coupling aryl or alkyl Grignard reagents and halogenated purine nucleosides in the presence of Fe(acac)3/CuI is described. A series of 6-substituted 7-deazapurines and the corresponding nucleosides were obtained in medium to good yields. For the synthesis of modified nucleosides that will be the subject of biological testing, we propose to use iron-catalyzed instead of palladium-catalyzed reaction. The synthesized compounds were tested for their antiproliferative activity. The cytotoxicity study of compounds 11a-q shows that by modifying the 6-position of 7-deazapurine ribonucleosides, the compounds may become selective for certain cancer cell lines.
PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES AS CGRP RECEPTOR ANTAGONISTS
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Page/Page column 39-40, (2009/07/25)
The present invention relates to novel compounds that are CGRP receptor antagonists, processes for their preparation, to compositions containing them and to their use in the treatment of migraine, headache, and cluster headache.
