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Nucleoside compound and preparation method thereof

A technology of compounds and nucleosides, which is applied in the field of nucleoside compounds and their preparation, and can solve problems such as the inactivation of xanthine nucleosides

Pending Publication Date: 2021-11-30
HARBIN UNIV OF COMMERCE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The present invention provides nucleoside compounds and their preparation methods to solve the problem in the prior art that cordycepin follows the purine nucleoside metabolic pathway in the body and is rapidly deaminated under the action of adenosine deaminase to become an inactive metabolite "3 '-deoxyinosine" and thus rapid inactivation defects

Method used

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  • Nucleoside compound and preparation method thereof
  • Nucleoside compound and preparation method thereof
  • Nucleoside compound and preparation method thereof

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preparation example Construction

[0042] In addition, this embodiment also provides a method for preparing nucleoside compounds, including: step 100, using 3'-deoxyadenosine nucleoside as a raw material, performing substituent protection to obtain a product one; step 200, the Product 1, introducing the target group to obtain Product 1; or, after the step 200 "introducing the target group to the product 1 to obtain Product 1", it also includes: Step 300, removing the product 1 Protection reaction to obtain product two; wherein, said product one or said product two are nucleoside compounds as described above.

[0043] As mentioned above, 3'-deoxyadenosine is the raw material drug-cordycepin. As mentioned above, step 100 is for the protection of 2'-OH and / or 5'-OH in 3'-deoxyadenosine nucleoside, and step 200 introduces the target group as for 6-NH 3 Substitution reactions of substituents introduce corresponding groups. Step 300 correspondingly removes the protection of 2'-OH and / or 5'-OH in step 100 to obtain ...

specific Embodiment approach 1

[0082] Further, specific embodiment 1: the antibacterial plane 112 includes a detachable substrate 1122, a gel layer 1123 disposed on the substrate, and a gel layer 1123 located away from the detachable substrate 1122. The microarray assembly 1124 on one side; the microarray assembly 1124 includes a plurality of microneedle monomers 1124a arranged at equal intervals on its surface; The drug delivery pipeline 1124-2 connected to the drug delivery thorn 1124a-1, and the inclusion gel 1124-3 coated on the periphery of the drug delivery pipeline 1124-2; the drug delivery thorn 1124a-1 And antibacterial components are set in the drug delivery pipeline 1124-2;

[0083] As mentioned above, the drug delivery puncture head 1124a-1 can pierce the cuticle of the human facial skin, and administer the drug into the skin cuticle, and the drug enters the skin through the drug delivery pipeline 1124-2 and the drug delivery thorn head 1124a-1, In order to achieve the antibacterial effect agai...

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Abstract

The invention provides a nucleoside compound and a preparation method thereof. The nucleoside compound comprises a compound as shown in a general formula, and pharmaceutically acceptable salts. According to the nucleoside compound, an amino substituent group at the sixth site of cordycepin is changed into aromatic substituent groups, such as p-methylthiophenyl, phenoxyl and p-methylaniline, so that a purine nucleoside metabolic pathway can be effectively avoided in vivo, the dosage concentration of the medicine is kept, the active effect of the medicine is fully exerted, and the defect that the generated medicine is quickly deaminated under the action of adenosine deaminase to become an inactive metabolite, namely 3'-deoxyinosine, is overcome.

Description

technical field [0001] The invention belongs to the technical field of drug synthesis, and in particular relates to nucleoside compounds and a preparation method thereof. Background technique [0002] Nucleosides are a class of water-soluble components with a wide range of physiological activities. As a nucleoside compound, cordycepin is also known as 3'-deoxyadenosine, and its chemical formula is C 10 h 13 N 5 o 3 . Cordycepin has been widely used as a terminator for DNA chain extension. Although in many cell experiments, cordycepin has a significant effect, after entering the body, most of it follows the purine nucleoside metabolic pathway. Under the action of ammonia enzyme (ADA), it is rapidly deaminated to become an inactive metabolite "3'-deoxyinosine" (Agarwal RP, Jr Biochem Pharmacol, 1975, 24 (6): 693-701 & 1977, 26 (5): 359-367), the specific deamination reaction is as follows: [0003] [0004] Fernandez-Noval A (Leroy F.J Endocrinology, 1979, 81 (3): 35...

Claims

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Application Information

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IPC IPC(8): C07H19/16C07H1/00A61P35/00A61P31/10A61K31/7076A41D13/11
CPCC07H19/16C07H1/00A61P35/00A61P31/10A41D13/1192
Inventor 申光焕崔琳琳
Owner HARBIN UNIV OF COMMERCE
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