Total synthesis of entecavir.

نویسندگان

  • Javier Velasco
  • Xavier Ariza
  • Laura Badía
  • Martí Bartra
  • Ramon Berenguer
  • Jaume Farràs
  • Joan Gallardo
  • Jordi Garcia
  • Yolanda Gasanz
چکیده

Entecavir (BMS-200475) was synthesized from 4-trimethylsilyl-3-butyn-2-one and acrolein. The key features of its preparation are: (i) a stereoselective boron-aldol reaction to afford the acyclic carbon skeleton of the methylenecylopentane moiety; (ii) its cyclization by a Cp2TiCl-catalyzed intramolecular radical addition of an epoxide to an alkyne; and (iii) the coupling with a purine derivative by a Mitsunobu reaction.

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عنوان ژورنال:
  • The Journal of organic chemistry

دوره 78 11  شماره 

صفحات  -

تاریخ انتشار 2013