- Preparation method of 1-(2-deoxy-beta-D-ribofuranose)-5-iodo-2-pyrimidone
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The invention relates to 1-(2-deoxidized-beta-D-ribofuranose)-5-iodo-2-pyrimidone, and particularly relates to a preparation method of 1-(2-deoxidized-beta-D-ribofuranose)-5-iodo-2-pyrimidone. The preparation method comprises the following steps of performing a reaction on 2-hydroxypyrimidine hydrochloride and a glacial acetic acid/iodine monochloride solution so as to generate 5-iodo-2-pyrimidone; performing a reaction on the 5-iodo-2-pyrimidone and 1-chloro-3,5-di(4-chlorbenzoyl)-2-deoxy-D-ribose so as to generate 1-[(3,5-di(4-chlorbenzoyl)-2-deoxy-beta-D-erythro-pentofuranose]-5-iodo-2-pyrimidone; and finally generating a target product by using the 1-[(3,5-di(4-chlorbenzoyl)-2-deoxy-beta-D-erythro-pentofuranose]-5-iodo-2-pyrimidone. All intermediates are stable, the yield is high, andthe method is suitable for industrial production.
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Paragraph 0070-0072; 0091-0096
(2018/04/01)
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- IDOXURIDINE AND ITS ANALOGS AS NEUROPROTECTANS FOR THE TREATMENT OF PARKINSONISM
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The invention relates to compounds that are useful in the treatment of parkinsonism, such as parkinsonism in connection with Parkinson's disease (PD); dementia with Lewy bodies (DLB); multiple system atrophy (MSA); corticobasal degeneration (CBD); or progressive supranuclear palsy (PSP). The said compounds include in particular idoxuridineand analogs thereofas well as their metabolic precursors, such as ropidoxuridine.The invention further relates to method for identifying compounds useful for the treatment of parkinsonism, said methods comprising detecting the capability of compound to increase the amount of GPR37 in cell membranes.The invention further relates to methods for the chemical synthesis of ropidoxuridine.
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Page/Page column 22; 27; 28
(2018/08/26)
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- Synthesis and Biological Activities of 2-Pyrimidinone Nucleosides. 2. 5-Halo-2-pyrimidinone 2'-Deoxyribonucleosides
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1-(2-Deoxy-β-D-ribofuranosyl)-5-bromo-2-pyrimidinone (BrPdR) and 1-(2-deoxy-β-D-ribofuranosyl)-5-iodo-2-pyrimidinone (IPdR) have been synthesized by condensation of the appropriate silylated bases 2a and 2b, respectively, with 3,5-bis-O-(p-chlorobenzoyl)-2-deoxy-α-D-ribofuranosyl chloride (8) in 1,2-dichloroethane, in the presence of SnCl4, followed by separation of the anomeric blocked nucleosides via column chromatography and subsequent deprotection with methanolic ammonia.Both BrPdR and IPdR exhibited significant antiherpes activities against various strains of HSV-1 and HSV-2, the latter compound (IPdR) showing the higher activity as well as the stronger binding to the virus-specific thimidine kinase.
- Efange, Simon M. N.,Alessi, Elaine M.,Shih, H. C.,Cheng, Yung-Chi,Bardos, Thomas J.
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p. 904 - 910
(2007/10/02)
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