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Synfacts 2010(2): 0145-0145
DOI: 10.1055/s-0029-1218517
DOI: 10.1055/s-0029-1218517
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag
Stuttgart ˙ New York
Synthesis of the Gastrin/CCK-B Receptor Antagonist (+)-AG-041R
S. Sato, M. Shibuya, N. Kanoh, Y. Iwabuchi*
Tohoku University, Sendai, Japan
Weitere Informationen
Publikationsverlauf
Publikationsdatum:
21. Januar 2010 (online)
Significance
AG-041R is an orally available gastrin/CCK-B antagonist that is a lead for the treatment of gastric ulcers. The synthesis depicted is noteworthy for the use of an asymmetric oxidative spiroannulation to construct the quaternary center in 3-aminooxindole structure C from the carbamate A using the rhodium catalyst B. For a related C-H insertion reaction, see: C. G. Espino, J. Du Bois Angew. Chem. Int. Ed. 2001, 40, 598.