1654021-72-3Relevant articles and documents
Multi-gram synthesis of a nucleotide-competing reverse transcriptase inhibitor
Duplessis, Martin,Morency, Louis,James, Clint,Minville, Joannie,Deroy, Patrick,Morin, Sébastien,Thavonekham, Bounkham,Tremblay, Martin,Halmos, Ted,Simoneau, Bruno,Bousquet, Yves,Sturino, Claudio
, p. 2303 - 2307 (2013)
An efficient multi-gram synthesis of a nucleotide-competing reverse transcriptase inhibitor is reported. The synthesis features a chiral auxiliary-assisted alcohol resolution, a Mitsunobu reaction involving a carbamate, followed by a lithium-iodide exchange/Weinreb ketone synthesis tandem. These chemical transformations were optimized in order to increase the yield of the synthesis. The route is concluded by a late-stage palladium-catalyzed cyanation followed by a pyrimidine-2-one ring formation.
