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Practical and Efficient Approach to the Preparation of Diquafosol Tetrasodium
Organic Process Research & Development ( IF 3.4 ) 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
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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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