Aminocarbonylation route to tolvaptan.
Pd-catalyzed aminocarbonylation between aryl bromide and NH-benzazepinone was effectively carried out to furnish the key intermediate for tolvaptan (up to 85%) in one step.
Torisawa
Yasuhiro
Y
Faculty of Pharmacy, Takasaki University of Health and Welfare, 60 Naka-Orui, Takasaki, Gunma 370-0033, Japan. torisawa@takasaki-u.ac.jp
Furuta
Takuya
T
Nishi
Takao
T
Aki
Shinji
S
Minamikawa
Jun-ichi
J
D001552:Benzazepines / Q000138:chemical synthesis*; D002384:Catalysis; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D010165:Palladium / Q000737:chemistry; D000077602:Tolvaptan; D014667:Vasopressins / Q000138:chemical synthesis
D001552:Benzazepines; D014667:Vasopressins; D000077602:Tolvaptan; D010165:Palladium