- RhII-catalyzed [3+2] cycloaddition of 2 H-azirines with N-sulfonyl-1,2,3-triazoles
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RhII-catalyzed intermolecular [3+2] cycloaddition of 2 H-azirines with N-sulfonyl-1,2,3-triazoles is disclosed, in which a series of fully functionalized pyrroles is produced via rhodium azavinyl carbene intermediates. A distinct feature of this reaction is that the azavinyl carbene serves as a [2 C] equivalent, instead of as [1 C] or aza-[3 C] synthons, which have been reported previously in cyclopropanations and [3 + n] cycloadditions. Moreover, this methodology has also been successfully applied in the total synthesis of URB447 as well as the formal synthesis of Atorvastatin (Lipitor).
- Zhao, Yun-Zhou,Yang, Hai-Bin,Tang, Xiang-Ying,Shi, Min
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supporting information
p. 3562 - 3566
(2015/03/04)
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- Synthesis and characterization of a peripherally restricted CB1 cannabinoid antagonist, URB447, that reduces feeding and body-weight gain in mice
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Cannabinoid CB1 receptor antagonists reduce body weight in rodents and humans, but their clinical utility as anti-obesity agents is limited by centrally mediated side effects. Here, we describe the first mixed CB1 antagonist/CB2
- LoVerme, Jesse,Duranti, Andrea,Tontini, Andrea,Spadoni, Gilberto,Mor, Marco,Rivara, Silvia,Stella, Nephi,Xu, Cong,Tarzia, Giorgio,Piomelli, Daniele
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experimental part
p. 639 - 643
(2009/09/06)
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