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Tandem RCM-isomerization-cyclopropanation reactions
Authors:Mallagaray Alvaro  Domínguez Gema  Gradillas Ana  Pérez-Castells Javier
Affiliation:Facultad de Farmacia, Dpto. Química, Universidad San Pablo CEU, Urb. Montepríncipe, ctra. Boadilla km 5,300 Boadilla del Monte, 28668 Madrid, Spain.
Abstract:A new triple tandem process has been discovered in which simple acyclic substrates can be transformed into bicyclic compounds via RCM-double bond isomerization-cyclopropanation. This process is catalyzed by second generation Grubb's catalyst without the requirement of other reactives or additives. In addition, a one-pot RCM-isomerization reaction followed by cyclopropanation with CHCl3/NaOH allows the synthesis of products related to iNOS (nitric oxide synthase) inhibitors, which are currently under clinical evaluation.
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