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Synfacts 2010(3): 0254-0254  
DOI: 10.1055/s-0029-1219292
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of the Gastrin/CCK-B Receptor Antagonist (+)-AG-041R

Contributor(s): Philip Kocienski
S. Sato, M. Shibuya, N. Katoh, Y. Iwabuchi*
Tohoku University, Sendai, Japan
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Publication History

Publication Date:
18 February 2010 (online)

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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.