143919-90-8Relevant articles and documents
Preparation method for emtricitabine isomer
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, (2019/04/26)
The invention discloses a preparation method for an embritabine isomer. The preparation method comprises the following steps: with Solketal as a starting material, allowing the Solketal to undergo a six-step reaction of esterification, hydrolysis, oxidation, condensation cyclization, acetylation and glycosylation condensation so as to synthesize four mixture intermediates of emtricitabine; and splitting the four isomer intermediates into a cis-isomer mixture and a trans-isomer mixture through a chiral reagent. According to the invention, by adoption of a simple starting material, a mixture forsplitting key intermediates of four optical isomers of the emtricitabine is synthesized through the six-step reaction, and chiral acid is utilized to split the four isomers into a mixture of cis andtrans isomers, so the preparation method provided by the invention has the advantages of simple and convenient operation, high yield and high isomer chiral purity.
Efficient asymmetric synthesis of lamivudine via enzymatic dynamic kinetic resolution
Hu, Lei,Schaufelberger, Fredrik,Zhang, Yan,Ramstroem, Olof
supporting information, p. 10376 - 10378 (2013/10/22)
The anti-HIV nucleoside lamivudine was asymmetrically synthesized in only three steps via a novel surfactant-treated subtilisin Carlsberg-catalyzed dynamic kinetic resolution protocol. The enantiomer of lamivudine could also be accessed using the same protocol catalyzed by Candida antarctica lipase B.
Facile preparation of α-acyloxyacetaldehyde, a versatile intermediate in the synthesis of antiviral nucleosides
Du, Jinfa,Watanabe, Kyoichi A.
, p. 1925 - 1930 (2007/10/03)
This report describes a novel and simple method for the preparation of a versatile intermediate, α-acyloxyacetaldehyde and its acetals, and its application to the synthesis of 4-acetoxy-2-acyloxymethyl-1,3-oxathiolane, an important intermediate in the syn