Tandem RCM-isomerization-cyclopropanation reactions |
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Authors: | Mallagaray Alvaro Domínguez Gema Gradillas Ana Pérez-Castells Javier |
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Affiliation: | Facultad de Farmacia, Dpto. Química, Universidad San Pablo CEU, Urb. Montepríncipe, ctra. Boadilla km 5,300 Boadilla del Monte, 28668 Madrid, Spain. |
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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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