1435752-55-8Relevant articles and documents
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.
PROCESS FOR PREPARING AN ANTIVIRAL DRUG AND INTERMEDIATES THEREOF
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, (2013/06/06)
Process for preparing an antiviral drug and intermediates thereof It comprises the preparation of entecavir of formula (I), or a pharmaceutically acceptable salt thereof, or a hydrate thereof by submitting a compound of formula (III) where X is an halogen selected from Cl, Br, and I, first to a hydrolysis reactionusing formic acid and then to a deprotection reaction, and isolating the entecavir either as free base or as a pharmaceutically acceptable salt. It also comprises intermediates which intervene in this preparation process.