Practical and Efficient Approach to the Preparation of Diquafosol Tetrasodium,Organic Process Research & Development

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Practical and Efficient Approach to the Preparation of Diquafosol Tetrasodium
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-06-30 , DOI: 10.1021/acs.oprd.0c00209
Pengfei Xu ₁ , Hai Wang ₂ , Pei Shen ₁ , Peng Peng ₂ , Yongrui Tu ₂ , Yongqiang Sun ₂ , Jubo Wang ₁ , Chenxi Xu ₁ , Zhixia Qiu ₁ , Raoling Ge ₃ , Zhiyu Li _{1,

4} , Jinlei Bian _{1,

4}

Affiliation

A scalable and practical route to synthesize the P2Y2 receptor agonist diquafosol tetrasodium has been described. Diquafosol tetrasodium was obtained via a four-step process starting from commercially available 5′-uridylic acid disodium salt. The whole procedure gives the target product in a 45% overall yield with high purity (>99%). Key steps in this process including isolation of impurities and the target product by using anion-exchange resin are discussed in detail. The optimized process has been successfully demonstrated on a large scale to support the development of diquafosol tetrasodium in China.

更新日期：2020-08-21

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