1435751-76-0Relevant academic research and scientific papers
Total synthesis of entecavir
Velasco, Javier,Ariza, Xavier,Badía, Laura,Bartra, Martí,Berenguer, Ramon,Farràs, Jaume,Gallardo, Joan,Garcia, Jordi,Gasanz, Yolanda
, p. 5482 - 5491 (2013/07/25)
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.
