An expedient route to a potent gastrin/CCK-B receptor antagonist (+)-AG-041R.
An enantiocontrolled synthesis of (+)-AG-041R (1), a potent gastrin/CCK-B receptor antagonist, has been achieved employing a chiral rhodium(II)-catalyzed, oxidative intramolecular aza-spiroannulation as the key step.
Sato
Shigeki
S
Graduate school of Pharmaceutical sciences, Tohoku University, 6-3 Aobayama, Sendai 980-8578, Japan.
Shibuya
Masatoshi
M
Kanoh
Naoki
N
Iwabuchi
Yoshiharu
Y
D002384:Catalysis; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D043887:Receptor, Cholecystokinin B / Q000037:antagonists & inhibitors; D012238:Rhodium / Q000737:chemistry; D013237:Stereoisomerism
C109755:AG-041R; D007211:Indoles; D043887:Receptor, Cholecystokinin B; D012238:Rhodium