Facile synthesis of the neuraminidase inhibitor peramivir

…, J Hong, PH Sun, JX Chen, WM Chen

Index: Jia, Fei; Hong, Juan; Sun, Ping-Hua; Chen, Jian-Xin; Chen, Wei-Min Synthetic Communications, 2013 , vol. 43, # 19 p. 2641 - 2647

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Citation Number: 6

Abstract

An improved and convenient synthetic route for the synthesis of peramivir has been developed with a total 34% yield. The process was improved from previous methods in three key reaction steps including 1,3-dipolar cycloaddition, reductive ring cleavage of the isoxazoline, and incorporation of the peripheral guanidino group. First, an activated sodium hypochlorite (Cl% = 10%) was employed for the catalytic 1,3-dipolar cycloaddition, and 61–68% yields were obtained. Second, the ...