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AssigneeBeijing Ribio Pharma Co., Ltd.
InventorsYazhou LI, Yibiao LIU, Guanshen ZHOU, Zhenchang CHEN, Hongjuan ZHANG
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The present disclosure provides a preparation method of a 2′-substituted pyrimidine nucleoside, including the following steps: subjecting a compound of Formula I or Formula II to a series of process including dehydration, selective 5′-protection, ring-opening reaction using magnesium alkoxide and deprotection to obtain a 2′-substituted pyrimidine nucleoside of Formula VII or Formula VIII. In the present disclosure, the preparation method has desirable universality for different substrates; the ring-opening with a protected anhydrous pyrimidine nucleoside improves a solubility of the substrate, with milder reaction conditions than those of a traditional synthetic route; the formation of a dimer is avoided during the ring-opening to improve the yield; in addition, an intermediate (5′-O-bis-p-methoxytrityl-protected 2′-substituted pyrimidine nucleoside) can be directly used in synthesis of a corresponding phosphoramidite monomer, with a wider potential for use.
1-13. (canceled)
A preparation method of a 2′-substituted pyrimidine nucleoside, comprising the following steps:
Dependencies are inferred from the claim text.